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Enzyme Nomenclature
Information on EC 3.4.21.73 - u-Plasminogen activator
for references in articles please use BRENDA:EC3.4.21.73
Word Map on EC 3.4.21.73
- 3.4.21.73
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fibrinolytic
- artery
- metastasis
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tissue-type
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thrombolysis
- vascular
- fibrin
- endothelial
- carcinoma
- clot
- vein
- inhibitor-1
- infarct
- heparin
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streptokinase
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catheter
- thrombus
- venous
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fibrinogen
- angiogenesis
- embolism
- myocardial
- coronary
- hemorrhage
- bleeding
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anticoagulation
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metalloproteinases
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single-chain
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zymography
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angiography
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angioplasty
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patency
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recanalization
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thrombotic
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vitronectin
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percutaneous
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intra-arterial
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thromboembolic
- occlusions
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transluminal
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intracoronary
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pericellular
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amidolytic
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thrombectomy
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kringle
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d-dimers
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reocclusion
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2-antiplasmin
- alteplase
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euglobulin
- agriculture
- diagnostics
- medicine
- pharmacology
- drug development
- analysis
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The enzyme appears in viruses and cellular organisms
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EC NUMBER 
COMMENTARY 
3.4.21.73
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RECOMMENDED NAME
GeneOntology No.
u-Plasminogen activator
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Specific cleavage of Arg-/-Val bond in plasminogen to form plasmin
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY
139639-24-0
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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29572, 29573, 29578, 29660, 29662, 29663, 29676, 667189, 667943, 668495, 668873, 668998, 669461, 669677, 670842, 670887, 670938, 683130, 683220, 683299, 683304, 683333, 683372, 683456, 683550, 683623, 683647, 683772, 684087, 694506, 695475, 695942, 696943, 697075, 697193, 697383, 697724, 697801, 698349, 699131, 699162, 699244, 699783, 700402, 700694, 701237, 701359, 701373, 707096, 707287, 707447, 707518, 707678, 707840, 707866, 707892, 707901, 707951, 707983, 708639, 708669, 708679, 708749, 708762, 708771, 709022, 709067, 709091, 709570, 709736, 709905, 709912, 710121, 710133, 710163, 710248, 710469, 710553, 710656, 717076, 717213, 717222, 717386, 717414, 717828, 717899, 717916, 718142, 718270, 718287, 731238, 731932, 732184
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UniProt
high-molecular weight uPA expressed in SP2/0 cell culture from Abbott Biotech; low-molecular weight uPA, Abbokinase, from Abbott Labs, North Chicago
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recombinant 54000 MW scuPA, plasmin-resistant rscuPA with Lys158 mutagenized to Glu and a 32000 MW form of rscuPA consisting of Leu144-Leu411 are obtained by expression of cDNA in Chinese hamster ovary cells
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recombinant plasmin-resistant mutant of single-chain uPA obtained by site-specific mutagenesis of Lys158 to Glu
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recombinant single chain urokinase-type plasminogen activator is home-made by expression of uPA cDNA in Chinese hamster ovary cells
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high-molecular weight uPA expressed in SP2/0 cell culture from Abbott Biotech; low-molecular weight uPA, Abbokinase, from Abbott Labs, North Chicago
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recombinant 54000 MW scuPA, plasmin-resistant rscuPA with Lys158 mutagenized to Glu and a 32000 MW form of rscuPA consisting of Leu144-Leu411 are obtained by expression of cDNA in Chinese hamster ovary cells
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recombinant single chain urokinase-type plasminogen activator is home-made by expression of uPA cDNA in Chinese hamster ovary cells
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29578, 668187, 668873, 669742, 683130, 683305, 683623, 683755, 684076, 695510, 695942, 696941, 698839, 707951, 710086, 717077, 717826, 717899, 731237, 731239, 731301, 731932, 732268, 732371, 732720
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mice model for kidney ischemia reperfusion injury and for acute kidney allograft rejection
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
metabolism
physiological function
additional information
malfunction
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urokinase plasminogen activator receptor, uPAR, deficient mice show reduced neutrophil recruitment and less severe lung injury during hyperoxia compared to wild-type mice, uPAR deficiency diminishes KC and IL-6 release and enhances activation of pulmonary coagulation, overview
malfunction
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urokinase plasminogen activator mediates impairment of hypercapnic and hypotensive cerebrovasodilation and pial artery dilation after cerebral hypoxia/ischemia, which is prevented by inhibition of integrin alphanubeta3, overview. Inhibition of uPA and integrin signaling may preserve cerebrohemodynamic control after hypoxia/ischemia
malfunction
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excessive fibrinolysis in monoclonal antibody light chain-amyloidosis is induced by urokinae-type plasminogen activator from bone marrow plasma cells, uPA expression analysis, overview
malfunction
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overexpression of uPAR promotes the invasive migration of hair follicle into the dermis in an uPA-dependent and an uPA-independent, ERK-dependent manner during human prenatal development
malfunction
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the urokinase plasminogen activating system is implicated in neoplastic progression and high tissue levels of uPAS components correlate with a poor prognosis in different human cancers
malfunction
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inhibition of u-PAR and u-PA attenuates lipopolysaccharid-mediated tumour cell adhesion and invasion
malfunction
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a wide variety of disorders are associated with an imbalance in the plasminogen activator system, including inflammatory diseases, atherosclerosis, intimal hyperplasia, the response mechanism to vascular injury, and restenosis. uPA is implicated in the stimulation of angiogenesis, detailed overview
malfunction
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a wide variety of disorders are associated with an imbalance in the plasminogen activator system, including inflammatory diseases, atherosclerosis, intimal hyperplasia, the response mechanism to vascular injury, and restenosis. uPA is implicated in the stimulation of angiogenesis, detailed overview
malfunction
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a wide variety of disorders are associated with an imbalance in the plasminogen activator system, including inflammatory diseases, atherosclerosis, intimal hyperplasia, the response mechanism to vascular injury, and restenosis. uPA is implicated in the stimulation of angiogenesis, detailed overview
malfunction
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uPA-dependent cleavage of alpha6integrin is involved in onset and progression of osseous metastases. Alpha6 integrin cleavage permits extravasation of human prostate cancer cells from circulation to bone and can be manipulated to prevent metastasis
malfunction
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uPA transcription and activity is only markedly increased during chronic neurodegeneration, not during acute intracerebral lipopolysaccharide-induced or acute kainate-induced neurodegeneration. Increase in total plasminogen activation with progression of prion disease is apparent in both soluble and membrane fractions
malfunction
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uPA is involved in adhesion, migration and invasion of hepatic Hep-G2 cancer cells, inhibition and downregulation of uPA by plumbagin also leads to inhibition of adhesion, migration and invasion by plumbagin in HepG2 cells, overview
malfunction
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pancreatic ductal adenocarcinoma, PDAC, expresses high levels of urokinase-type plasminogen activator, its receptor uPAR, and plasminogen activator inhibitor-2, which may play an important role in PDAC progression. Proliferation and migration of pancreatic adenocarcinoma cells via regulation of ERK/p38 signaling is inhibited by suppression of urokinase plasminogen activator receptor. Effects of uPAR in the uPA system on cancer cell development and progression, overview
malfunction
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urokinase-type plasminogen activator receptor, u-PAR, is overexpressed in many human malignant tumors including oral squamous cell carcinoma and plays an important role in a variety of cancer key cellular events as a versatile signaling orchestrator. MMP-9, MMP-2 and u-PA enzymatic activities are significantly reduced in u-PAR-specific siRNA cells. RNAi targeting u-PAR can effectively inhibit the metastasis and progression of oral squamous cell carcinoma in vivo
malfunction
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upregulation of the uPA system is correlated with malignancy of various carcinomas
malfunction
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binding of urokinase-type plasminogen activator, uPA, to the uPA receptor, uPAR, existing on the surface of cancer cell is considered to be a trigger for cancer invasions
malfunction
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uPA stimulates glioblastoma multiforme cell invasiveness, in sphingosine-1-phosphate-induced invasion using a spheroid invasion assay
malfunction
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uPA overexpression in brain cortex and hippocampus is involved in epileptic pathology
malfunction
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uPA is involved in cell invasion of breast cancer cells, uPA is a key regulator of breast cancer invasion and metastasis, overview
malfunction
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uPA is an important protease believed responsible for several tumour characteristics through its activation of certain proteases and growth factors. uPA is essential in the degradation of peritumour extracellular matrix. uPA, induced by PGE2 from stromal fibroblasts surrounding lung tumour, thus appears to play an important role through EP receptors
malfunction
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at pathophysiological concentrations above 20 nM, uPA inhibits contractility and increases vascular permeability
malfunction
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macrophage-specific uPA overexpression accelerates atherosclerosis and causes aortic root dilation in fat-fed Ldlr-/-mice. Macrophage-expressed uPA accelerates atherosclerosis by stimulation of lesion progression rather than initiation and causes disproportionate lipid accumulation in early lesions. uPA-accelerated atherosclerosis and aortic dilation are largely, if not completely, independent of uPA receptor, uPAR. In the absence of uPA overexpression, however, uPAR contributes modestly to both atherosclerosis and aortic dilation
malfunction
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livers of uPA-ablated mice elevated TIMP-1 levels do not trigger HGF signalling and do not promote metastasis of a murine T-lymphoma cell line, decreased TIMP-1-induced tumour cell scattering in uPA knockout mice. In contrast, lack of tumour cell-derived uPA induced by gene silencing do not interfere with this pro-metastatic pathway
malfunction
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in enzyme knockout mice, the number of peritoneal macrophages is lower by 30% than the peritoneal macrophages harvested from wild-type C57BL/6 mice
malfunction
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enzyme receptor defciient mice show no lipid droplets in their livers compared to wild-type C57BL/6 mice and the triglyceride levels are significantly lower, phenotype, overview
malfunction
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macrophage adhesion to vitronectin is blocked by plasminogen activator inhibitor-1, which is also able to enhance in turn the two-dimensional migration on this matrix protein
malfunction
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genetic deficiency of enzyme or urokinase plasminogen activator receptor abrogates functional recovery after acute ischemic stroke
malfunction
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suppression of uPA retards development of pancreatic cancer in nude mice and increases sensitization to gemcitabine
malfunction
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overexpression of urokinase plasminogen activator in macrophages induces spontaneous macrophage accumulation and fibrosis specific to the heart in mice
malfunction
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both C57/black 6J, and AlbPLG1 mice expressing the human plasminogen transgene, are significantly more susceptible to invasive Group A Streptococcus strain 5448 disease than enzyme-deficient uPA-/- mice. The observed decrease in virulence in uPA-/- mice correlates directly with a decrease in bacterial dissemination and reduced cell surface plasmin accumulation by Group A Streptococci
malfunction
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enzyme receptor defciient mice show no lipid droplets in their livers compared to wild-type C57BL/6 mice and the triglyceride levels are significantly lower, phenotype, overview; in enzyme knockout mice, the number of peritoneal macrophages is lower by 30% than the peritoneal macrophages harvested from wild-type C57BL/6 mice; macrophage adhesion to vitronectin is blocked by plasminogen activator inhibitor-1, which is also able to enhance in turn the two-dimensional migration on this matrix protein; macrophage-specific uPA overexpression accelerates atherosclerosis and causes aortic root dilation in fat-fed Ldlr-/-mice. Macrophage-expressed uPA accelerates atherosclerosis by stimulation of lesion progression rather than initiation and causes disproportionate lipid accumulation in early lesions. uPA-accelerated atherosclerosis and aortic dilation are largely, if not completely, independent of uPA receptor, uPAR. In the absence of uPA overexpression, however, uPAR contributes modestly to both atherosclerosis and aortic dilation; uPA transcription and activity is only markedly increased during chronic neurodegeneration, not during acute intracerebral lipopolysaccharide-induced or acute kainate-induced neurodegeneration. Increase in total plasminogen activation with progression of prion disease is apparent in both soluble and membrane fractions; urokinase plasminogen activator receptor, uPAR, deficient mice show reduced neutrophil recruitment and less severe lung injury during hyperoxia compared to wild-type mice, uPAR deficiency diminishes KC and IL-6 release and enhances activation of pulmonary coagulation, overview
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malfunction
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genetic deficiency of enzyme or urokinase plasminogen activator receptor abrogates functional recovery after acute ischemic stroke
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metabolism
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involvement of the uPAR/uPA system in CNS function and pathology, overview
metabolism
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the enzyme uPA is a serine protease, and together with its membraneassociated receptor uPAR, is part of the uPA/uPAR system, which is an important component of the fibrinolytic system
metabolism
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the urokinase plasminogen activation pathways are comprised of urokinase-type plasminogen activator, its plasmalemmal receptor, and extracellular plasminogen
metabolism
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a poor prognosis of pancreatic ductal adenocarcinoma is correlated with increased expression of urokinase plasminogen activator
metabolism
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involvement of the uPAR/uPA system in CNS function and pathology, overview
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physiological function
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uPA is a potent catalyst of extracellular proteolysis and manifests this action through the conversion of plasminogen into plasmin, which has a range of specificities
physiological function
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the plasminogen system plays a crucial role in the repair of a variety of tissues, including skeletal muscle. uPA promotes muscle regeneration by activating hepatocyte growth factor, which, in turn, stimulates proliferation of myoblasts required for regeneration. uPA promotes myoblast proliferation in vitro through its proteolytic activity
physiological function
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uPA is a multifunctional protein that in addition to its fibrinolytic and matrix degradation capabilities also affects growth factor bioavailability, cytokine modulation, receptor shedding, cell migration and proliferation, phenotypic modulation, protein expression, and cascade activation of proteases, inhibitors, receptors, and modulators. uPA is the crucial protein for neointimal growth and vascular remodeling. Mechanism of fibroblast-to-myofibroblast transformation induced by uPA. Detailed overview
physiological function
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uPA is a multifunctional protein that in addition to its fibrinolytic and matrix degradation capabilities also affects growth factor bioavailability, cytokine modulation, receptor shedding, cell migration and proliferation, phenotypic modulation, protein expression, and cascade activation of proteases, inhibitors, receptors, and modulators. uPA is the crucial protein for neointimal growth and vascular remodeling. Mechanism of fibroblast-to-myofibroblast transformation induced by uPA. Detailed overview
physiological function
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uPA is a multifunctional protein that in addition to its fibrinolytic and matrix degradation capabilities also affects growth factor bioavailability, cytokine modulation, receptor shedding, cell migration and proliferation, phenotypic modulation, protein expression, and cascade activation of proteases, inhibitors, receptors, and modulators. uPA is the crucial protein for neointimal growth and vascular remodeling. Mechanism of fibroblast-to-myofibroblast transformation induced by uPA. Detailed overview
physiological function
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uPA binds to the urokinase receptor, uPAR, expressed on the surface of many cell types, that coordinates plasmin-mediated cell surface proteolysis for matrix remodeling and promotes cell adhesion by acting as a binding protein for vitronectin. Role of uPAR in the phagocytosis of apoptotic cells, a process termed efferocytosis, overview
physiological function
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the uPA-uPA receptor, uPAR, system plays a critical role in the regulation of cancer cell migration, extracellular matrix invasion, and metastasis. uPA binds with high affinity to a cell surface uPAR, that is a heavily glycosylated glycosylphosphatidylinositol-anchored protein formed by three cysteine-rich LY6-like extracellular domains. uPA-uPAR promotes extracellular proteolysis by regulating plasminogen activation, uPA-uPAR regulates cell-extracellular matrix interactions as an adhesion receptor for vitronectin and through its capacity to modulate integrin function, and uPA-uPAR regulates cell migration as a signal transduction molecule and by its intrinsic chemotactic activity. Src/MAP kinase, but not FAK and PI3K, is involved in ECRG2-regulated, uPA-dependent cell migration/invasion
physiological function
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urokinase plasminogen activator receptor, u-PAR, binds u-PA and participates in plasminogen activation in addition to modulating several cellular processes such as adhesion, proliferation, and migration
physiological function
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urokinase-type plasminogen activator induces BV-2 microglial cell migration through activation of matrix metalloproteinase-9
physiological function
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uPA elicits various cellular responses, involving the activation of distinct signaling pathways
physiological function
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the urokinase plasminogen activator, uPA, system, comprising of uPA, its receptor uPAR and inhibitor, type 1 plasminogen activator inhibitor, PAI-1, plays a vital role in various biological processes involving extracellular proteolysis, fibrinolysis, cell migration and proliferation
physiological function
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uPA limits the accretion of fibrin after lung injury. uPA regulates the in vitro pulmonary arterial contractility induced by phenylephrine in a dose-dependent manner through two receptor-dependent pathways, and regulates vascular contractility and permeability in vivo. Physiological concentrations of uPA below 1 nM stimulate the contractility of pulmonary arterial rings induced by phenylephrine through the low-density lipoprotein receptor-related protein receptor. The pro-contractile effect of uPA is independent of its catalytic activity. The inhibition of vascular contractility and increase of vascular permeability is mediated through a two-step process that involves docking to N-methyl-Daspartate receptor-1 on pulmonary vascular smooth muscle cells, and requires catalytic activity
physiological function
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urokinase-type plasminogen activator is involved in diverse physiologic and pathophysiologic processes, including fibrinolysis, cell migration and adhesion, and inflammation, thereby playing a role in efferocytosis. uPA inhibits the uptake of apoptotic neutrophils, suggest a novel mechanism by which elevated levels of uPA may participate in enhancing the duration and severity of inflammatory processes, such as acute lung injury. The phagocytosis of apoptotic neutrophils by macrophages is significantly inhibited by uPA, the process requires the kringle domain of uPA, and involves alphaVbeta3 integrin and vitronectin. But protease activity is not required for uPA to inhibit the engulfment of apoptotic neutrophils by macrophages, overview. Wild-type and inactive uPA are able to inhibit phagocytosis of apoptotic neutrophils by macrophages
physiological function
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plasmin and urokinase-type plasminogen activator are ubiquitous proteases that regulate the extracellular environment and activate each other through proteolytic cleavage. Although neither plasmin nor urokinase-type plasminogen activator exhibit allosteric cooperativity, modeling shows that cooperativity occurs at the system level because of substrate competition, computational simulations and bifurcation analysis, overview. Ultrasensitive, bistable activation of UPA-PLS is possible in the presence of substrate competition
physiological function
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the urokinase plasminogen activator system is implicated in cell migration and cancer metastasis
physiological function
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the urokinase plasminogen activator/uPA receptor/plasminogen system is involved in the development of atherosclerosis and aneurysms, modeling, overview
physiological function
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two-chain active uPA and uPA-PAI-1 enzyme-inhibitor complex induce phosphorylation of endothelial NOS-Ser1177 in pulmonary microvascular endothelial cells, which is followed by generation of NO and the nitrosylation and dissociation of beta-catenin from VE-cadherin, mechanism of uPA-induced pulmonary vascular permeability in vivo, overview. Effects of uPA-PAI-1 are abrogated by the nitric-oxide synthase inhibitor N-D-nitro-L-arginine methyl ester. The PI3K/Akt pathway is not essential for uPA-induced phosphorylation of eNOS
physiological function
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plasminogen activator, together with urokinase-type plasminogen activator inhibitor-1, PAI-1, plays a pivotal role in fibrinolysis, cell migration, and tissue remodeling
physiological function
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uPA is a crucial protagonist for the tissue inhibitor of metalloproteinases-1, TIMP-1, induced modulation of a pro-metastatic microenvironment in the liver of mice. Elevated levels of TIMP-1 render the liver more susceptible to metastasis by triggering urokinase plasminogen activator expression as well as hepatocyte growth factor signalling, thereby leading to the fatal scattered infiltration of metastasizing tumour cells throughout the parenchyma of the target organ. Host uPA is necessary for the recruitment of neutrophilic granulocytes and the associated increase of HGF in livers with elevated TIMP-1 levels
physiological function
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uPA is a crucial protagonist for the tissue inhibitor of metalloproteinases-1, TIMP-1, induced modulation of a pro-metastatic microenvironment in the liver of mice. Elevated levels of TIMP-1 render the liver more susceptible to metastasis by triggering urokinase plasminogen activator expression as well as hepatocyte growth factor signalling, thereby leading to the fatal scattered infiltration of metastasizing tumour cells throughout the parenchyma of the target organ. Host uPA is necessary for the recruitment of neutrophilic granulocytes and the associated increase of HGF in livers with elevated TIMP-1 levels
physiological function
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urokinase-type plasminogen activator is a protease involved in tissue remodeling and cell migration, increased expression of uPA in pterygium may covert plasminogen to plasmin, degrade extracellular matrixes, stimulate cell migration, induce angiogenesis, and plays an important role in the development and progression of pterygium
physiological function
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urokinase plasminogen activator inhibits HIV virion release from macrophage-differentiated chronically infected cells via activation of RhoA and PKCepsilon. Interaction of urokinase-type plasminogen activator with its cell surface receptor favours virion accumulation in such subcellular compartment in primary monocyte-derived macrophages and chronically infected promonocytic U1 cells differentiated into macrophage-like cells by stimulation with phorbol myristate acetate, PMA, uPA induces actin rearrangement in PMA stimulated U1 cells. uPA/uPAR interaction leads to the redirection of virion accumulation in intra-cytoplasmic vesicles. Anti-HIV effect of uPA is mediated by RhoA and PKCepsilon, but not by PKCdelta. uPA induces activation of RhoA, and of PKC epsilon and delta isoforms
physiological function
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the enzyme modulates monocyte-to-macrophage differentiation and prevents oxidized LDL-induced macrophage apoptosis via ERK1/2 activation-dependent Bim downregulation, mechanism, overview. The enzyme attenuates MonoMac6 macrophage-like cell line apoptosis (with maximal inhibition of 51% by 5 nmol/l of enzyme) induced by oxidized LDL and by thapsigargin (inhibitor of sarcoendoplasmic reticulum Ca2þ-ATPase), but not by staurosporine (protein kinase inhibitor), suggesting that the enzyme's antiapoptotic activity is Ca2+-independent, but involves a kinase activation. Monocyte-to-macrophage differentiation and macrophage death play a pivotal role in atherogenesis. The enzyme and its receptor uPAR are expressed in atherosclerotic lesion macrophages and contribute to atherosclerosis progression. The enzyme attenuates endoplasmatic reticulum stress-induced cell death, overview
physiological function
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the enzyme modulates monocyte-to-macrophage differentiation and prevents oxidized LDL-induced macrophage apoptosis via ERK1/2 activation-dependent Bim downregulation, mechanism, overview. Monocyte-to-macrophage differentiation and macrophage death play a pivotal role in atherogenesis. The enzyme and its receptor uPAR are expressed in atherosclerotic lesion macrophages and contribute to atherosclerosis progression
physiological function
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increasing concentrations of the enzyme dose-dependently decrease SR-BI protein expression in the liver and Huh-7 hepatoma cell line..The enzyme decreases both the cellular binding of HDL to Huh-7 hepatocytes, and the selective uptake of HDL-cholesteryl ester from HDL, it decreases the removal of HDL-cholesteryl ester in the liver via suppression of the hepatic SR-BI expression
physiological function
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the urokinase-type plasminogen activator regulates gene expression in the liver involving peroxisome-proliferator-activated receptor gamma's transcriptional activity and stimulates triglyceride synthesis in Huh-7 hepatoma cells via p38-dependent upregulation of diglyceride acyltransferase 2. Also, the amount of free fatty acids is highly up regulated by the enzyme through activation of the transcription factor SREBP-1., overview
physiological function
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the enzyme mediates interleukin-17-induced peripheral blood mesenchymal stem cell motility and transendothelial migration without affecting matrix metalloproteinase expression, detailed overview. Interleukin-17 increases peripheral blood mesenchymal stem cell adhesion to endothelial cells and transendothelial migration, as well as increases the capacity of cell adhesion to fibronectin, in an urokinase-tyype plasminogen activator-dependent fashion
physiological function
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activated extracellular enzyme cleaves plasminogen to plasmin, which initiates an extracellular protease cascade to degrade the extracellular matrix and facilitate cellular processes such as cellular migration, angiogenesis, tissue remodeling, and wound repair
physiological function
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activation of alphabetagamma-epithelial sodium channel specifically by the enzyme may contribute to fluid clearance under physiological conditions and in injured tissues, multifaceted mechanisms for enzyme-mediated up-regulation of the epithelial sodium channel, which form the cellular and molecular rational for the beneficial effects of urokinase in mitigating mortal pulmonary edema and pleural effusions, overview
physiological function
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urokinase plasminogen activator and its receptor coordinate a plasmin-mediated proteolytic cascade that is implicated in cell adhesion, cell motility, and matrix breakdown, for example, during inflammation. The enzyme is a central regulator of macrophage three-dimensional invasion, matrix degradation, and adhesion. Macrophage adhesion to vitronectin is enhanced by the enzyme. The enzyme's proteolytic activity is required for optimal macrophage three-dimensional invasion through a matrix barrier
physiological function
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urokinase-type plasminogen activator is a serine protease that is implicated as a key mediator of cellular invasion and tissue remodeling, the enzyme is thought to play a central role in tumor metastasis and angiogenesis
physiological function
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urokinase-type plasminogen activator is a serine proteinase that plays a central role in tissue remodeling via binding to the urokinase plasminogen activator receptor and promotes dendritic spine recovery and improves neurological outcome following ischemic stroke. The enzyme does not have an effect on ischemia- or hypoxia-induced neuronal death. The excitotoxic injury induces the clustering of enzyme receptor in dendritic varicosities, and the binding of the enzyme and its receptor promotes the reorganization of the actin cytoskeleton and re-emergence of dendritic filopodia from enzyme receptor-enriched varicosities mediated by Rac-regulated profilin expression and cofilin phosphorylation
physiological function
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role of the enzyme in pancreatic ductal adenocarcinoma cancer stem cells, a large fraction of these side population cells are CD44 and CD24 positive, are gemcitabine resistant, possess sphere-forming ability, and exhibit increased tumorigenicity. The enzyme interacts directly with transcription factors LIM homeobox-2 (Lhx2), homeobox transcription factor A5 (HOXA5), and Hey to possibly promote cancer stemness. The enzyme regulates Lhx2 expression by suppressing expression of miR-124 and p53 expression by repressing its promoter by inactivating HOXA5. Regulation of gene transcription by the enzyme contributes to cancer stemness and clinical lethality
physiological function
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the enzyme plays an important role in the processes of tumor cell metastasis, aortic aneurysm, and multiple sclerosis
physiological function
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urokinase plasminogen activator induces pro-fibrotic/m2 phenotype in murine cardiac macrophages, overview. The phenotype is adopted after migration of the macrophages to the heart. Elevation of the pro-inflammatory cytokine interleukin-6 in hearts of transgenic mice overexpressing the enzyme, interleukin-6 is not a major effector of the enzyme-induced cardiac fibrosis
physiological function
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the enzyme is primarily involved in cell-associated plasminogen activation. Urokinase-type plasminogen activator contributes to plasmin recruitment and subsequent invasive disease initiation by invasive Group A streptococci in vivo, it hhas a key role in cell surface plasmin acquisition and bacterial dissemination in invasive Group A streptococcus disease
physiological function
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the enzyme modulates monocyte-to-macrophage differentiation and prevents oxidized LDL-induced macrophage apoptosis via ERK1/2 activation-dependent Bim downregulation, mechanism, overview. Monocyte-to-macrophage differentiation and macrophage death play a pivotal role in atherogenesis. The enzyme and its receptor uPAR are expressed in atherosclerotic lesion macrophages and contribute to atherosclerosis progression; the plasminogen system plays a crucial role in the repair of a variety of tissues, including skeletal muscle. uPA promotes muscle regeneration by activating hepatocyte growth factor, which, in turn, stimulates proliferation of myoblasts required for regeneration. uPA promotes myoblast proliferation in vitro through its proteolytic activity; the urokinase plasminogen activator/uPA receptor/plasminogen system is involved in the development of atherosclerosis and aneurysms, modeling, overview; urokinase plasminogen activator and its receptor coordinate a plasmin-mediated proteolytic cascade that is implicated in cell adhesion, cell motility, and matrix breakdown, for example, during inflammation. The enzyme is a central regulator of macrophage three-dimensional invasion, matrix degradation, and adhesion. Macrophage adhesion to vitronectin is enhanced by the enzyme. The enzyme's proteolytic activity is required for optimal macrophage three-dimensional invasion through a matrix barrier; urokinase-type plasminogen activator is involved in diverse physiologic and pathophysiologic processes, including fibrinolysis, cell migration and adhesion, and inflammation, thereby playing a role in efferocytosis. uPA inhibits the uptake of apoptotic neutrophils, suggest a novel mechanism by which elevated levels of uPA may participate in enhancing the duration and severity of inflammatory processes, such as acute lung injury. The phagocytosis of apoptotic neutrophils by macrophages is significantly inhibited by uPA, the process requires the kringle domain of uPA, and involves alphaVbeta3 integrin and vitronectin. But protease activity is not required for uPA to inhibit the engulfment of apoptotic neutrophils by macrophages, overview. Wild-type and inactive uPA are able to inhibit phagocytosis of apoptotic neutrophils by macrophages
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physiological function
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urokinase-type plasminogen activator is a serine proteinase that plays a central role in tissue remodeling via binding to the urokinase plasminogen activator receptor and promotes dendritic spine recovery and improves neurological outcome following ischemic stroke. The enzyme does not have an effect on ischemia- or hypoxia-induced neuronal death. The excitotoxic injury induces the clustering of enzyme receptor in dendritic varicosities, and the binding of the enzyme and its receptor promotes the reorganization of the actin cytoskeleton and re-emergence of dendritic filopodia from enzyme receptor-enriched varicosities mediated by Rac-regulated profilin expression and cofilin phosphorylation
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additional information
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uPAR is a key receptor involved in the formation of the serine protease plasmin by interacting with uPA and has been implicated in many physiological processes including proliferation and migration, determination of key regulatory regions and splice variants of UPAR, of multiple forms of uPAR, overview
additional information
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lipopolysaccharide promotes tumour cell ECM adhesion and invasion through activation of the u-PA system in a TLR-4- and NF-kappaB-dependent manner, overview
additional information
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plasminogen activators are serine proteases that are classified as either urokinase-type PA, uPA, or tissue-type PA, tPA, based on their molecular mass
additional information
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development of specific monoclonal antibodies against uPA able to detect the enzyme in tumor cell surfaces, overview
additional information
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sphingosine kinase is necessary for basal activity of the uPA system and glioma cell invasion, while sphingosine 1-phosphate receptor signaling enhances invasion, partially through uPA and CCN1
additional information
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the expression and release of uPA is under active regulation in BV2 microglial cells
additional information
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urokinase plasminogen activator is elevated in pathological settings such as acute lung injury, where pulmonary arterial contractility and permeability are disrupted
additional information
-
LasB, a thermolysin-like metalloprotease secreted by Pseudomonas aeruginosa, converts the human uPA zymogen into its active form, processes the uPA receptor, inactivates the plasminogen activator inhibitor 1, and activates pro-matrix metalloproteinase 2
additional information
-
there exists a direct link between conformational changes of the autolysis loop and the creation of a catalytically mature active site. The conformation-specific antibodies mAb-112 and mAb-12E6B10 are useful to selectively stain pro-uPA or active uPA on the surface of cultured cells
additional information
-
concept of the protease web as the complex interplay between proteinases, their inhibitors and effector molecules, overview
additional information
-
chemotherapy prevents osteosarcoma cell invasion by down-regulation of urokinase plasminogen activity via up-regulation of transcription factor early growth response 1, EGR1, during chemotherapy period, overview
additional information
-
the catalytic activity of serine proteases depends on a salt-bridge between the amino group of residue 16 and the side chain of Asp194. The salt-bridge stabilizes the oxyanion hole and the S1 specificity pocket of the protease. Some serine proteases exist in only partially active forms, in which the amino group of residue 16 is exposed to the solvent. Such a partially active state is assumed by a truncated form of the murine urokinase-type plasminogen activator consisting of residues 16-243, allosteric interconversion analysis between partially active states and the fully active state, overview. Both a monoclonal antibody (mU3) and a peptidic inhibitor (mupain-1-16) stabilize the active state
additional information
-
highly invasive cancers of breast, brain, prostate and lung notably have increased levels of the enzyme, its receptor uPAR, or an endogenous inhibitor protein PAI-1, which correlate with the propensity of a cancer cell type to invade and to disseminate
additional information
-
the enzyme's catalytic domain comprises residues 159-411
additional information
-
the enzyme's catalytic domain comprises residues 159-411
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
benzoyl-beta-Ala-Gly-Arg-4-nitroanilide + H2O
benzoyl-beta-Ala-Gly-Arg + 4-nitroaniline
-
-
-
-
?
Cellular receptor of urokinase-type plasminogen activator + H2O
?
-
cleavage between domains 1 and 2 generating a cell-associated variant of the receptor of urokinase-type plasminogen activator without ligand-binding properties, uPA catalyzed cleavage does not require binding of the protease to the receptor through its epidermal growth factor-like receptor-binding domain, low-molecular weight uPA lacking this domain also cleaves the substrate
-
-
-
D-Glu-Gly-Arg-4-nitroanilide + H2O
D-Glu-Gly-Arg + 4-nitroaniline
-
a uPA substrate S-2444
-
-
?
epithelial sodium channel gamma subunit + H2O
?
-
of Xenopus laevis ocytes, activation by proteolytic cleavage at 177GR-/-KR180
-
-
?
L-diglutamyl-glycyl-L-arginine 4-nitroanilide + H2O
L-diglutamyl-glycyl-L-arginine + 4-nitroaniline
-
-
-
-
?
L-pyroglutamyl-glycyl-L-arginine-p-nitroanilide + H2O
L-pyroglutamyl-glycyl-L-arginine + 4-nitroaniline
-
-
-
?
N-benzyloxycarbonyl-Gly-Gly-Arg-7-amido-4-trifluoromethylcoumarin + H2O
N-benzyloxycarbonyl-Gly-Gly-Arg + 7-amino-4-trifluoromethylcoumarin
-
-
-
-
-
pyro-Glu-Pro-Arg-4-nitroanilide + H2O
pyro-Glu-Pro-Arg + 4-nitroaniline
-
-
-
-
?
pyroGlu-Gly-Arg-4-nitroanilide + H2O
pyroGlu-Gly-Arg + 4-nitroaniline
-
i.e. S-2444, a chromogenic substrate
-
-
?
S2444 + H2O
pyroGlu-Gly-Arg + 4-nitroaniline
-
i.e. 5-oxo-L-Pro-Gly-L-Arg-p-nitroanilide
-
?
t-butyloxycarbonyl-valyl-leucyl-lysine-4-methylcoumaryl-7-amide + H2O
Boc-L-Val-L-Leu-L-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
alpha6 integrin + H2O
?
-
alpha6 integrin is present on prostate carcinoma escaping the gland via nerves. Urokinase-dependent cleavage of the laminin binding domain from the prostate tumor cell surface
-
-
?
L-pyroGlu-Gly-L-Arg-4-nitroanilide + H2O
L-pyroGlu-Gly-L-Arg + 4-nitroaniline
-
i.e. S-2444
-
-
?
L-pyroGlu-Gly-L-Arg-4-nitroanilide + H2O
L-pyroGlu-Gly-L-Arg + 4-nitroaniline
-
chromogenic substrate S-2444
-
-
?
plasminogen + H2O
?
-
the enzyme mediates pericellular proteolysis during cell migration and tissue remodelling under physiological and pathophysiological conditions
-
-
-
plasminogen + H2O
?
-
potential role for uPA is a direct regulation of metalloproteinases-mediated extracellular proteolysis via the cleavage of the 72000 MW gelatinase/type IV collagenase to an 62000 MW form
-
-
-
plasminogen + H2O
?
-
key enzyme in the thrombolytic cascade converting plasminogen into plasmin, which in turn degrades thrombus fibrin
-
-
-
plasminogen + H2O
?
-
the enzyme promotes fibrinolysis by catalyzing the conversion of plasminogen to plasmin
-
-
-
plasminogen + H2O
?
-
when localized to the external cell surface it contributes to tissue remodelling and cellular migration
-
-
-
plasminogen + H2O
?
-
the enzyme is responsible for plasminogen activation, it is also involved in cell adhesion, chemotaxis, and proliferation, the signaling events are not mediated by uPA receptor uPAR/CD87, but require the kringle domain of the enzyme, which binds integrin alphanybeta3 for induction of cell migration, e.g. of CHO cells, overview
-
-
?
plasminogen + H2O
plasmin + ?
-
-
669677, 683130, 683220, 683299, 683456, 683550, 683623, 707518, 707866, 707901, 707951, 708639, 709091, 709905, 710248, 717213, 717386, 717916, 718142, 731365, 731429, 732801
-
-
?
plasminogen + H2O
plasmin + ?
-
-
generation of 2 polypeptides, one of 80000 MW (A-chain), and the other of 27000 MW (B-chain)
-
plasminogen + H2O
plasmin + ?
-
Glu-plasminogen, the native form of human plasminogen
-
-
plasminogen + H2O
plasmin + ?
-
principal function is fibrinolysis, u-PA also been implicated in other physiological functions such as embryogenesis, cell migration, tissue remodeling, ovulation, and wound healing
-
?
plasminogen + H2O
plasmin + ?
-
hearts with end-stage failure and fibrosis have macrophage accumulation and elevated plasminogen activator activity, mechanisms that link macrophage accumulation and plasminogen activator activity with cardiac fibrosis, dependent on localization of uPA by the uPA receptor uPAR, on activation of plasminogen by uPA and subsequent activation of transforming growth factor-beta1 and matrix metalloproteinase MMP-2 and MMP-9 by plasmin, overview, uPA-induced cardiac fibrosis can be attenuated by treatment with verapamil, plasminogen is necessary for uPA-induced cardiac fibrosis and macrophage accumulation, but uPAR is not
-
-
?
plasminogen + H2O
plasmin + ?
-
the uPA proteolytic domain specifically cleaves plasminogen and converts it into the serine protease plasmin with wide substrate specificity. Plasmin directly degrades fibrin, leading to thrombus dissolution and activating a number of matrix metalloproteinases
-
-
?
plasminogen + H2O
plasmin + ?
-
u-PA forms a complex with its receptor u-PAR in plasminogen ativation
-
-
?
plasminogen + H2O
plasmin + ?
-
casein-plasminogen zymography assay method
-
-
?
plasminogen + H2O
plasmin + ?
-
-
-
-
?
plasminogen + H2O
plasmin + ?
-
Glu-plasminogen, the native form of human plasminogen
-
-
plasminogen + H2O
plasmin + ?
-
the urokinase-type and tissue-type plasminogen activators regulate liver matrix remodelling through the conversion of plasminogen to the active protease plasmin, uPA is bound to its receptor uPAR, overview
-
-
?
plasminogen + H2O
plasmin + ?
-
the uPA proteolytic domain specifically cleaves plasminogen and converts it into the serine protease plasmin with wide substrate specificity. Plasmin directly degrades fibrin, leading to thrombus dissolution and activating a number of matrix metalloproteinases
-
-
?
plasminogen + H2O
plasmin + ?
-
the uPA proteolytic domain specifically cleaves plasminogen and converts it into the serine protease plasmin with wide substrate specificity. Plasmin directly degrades fibrin, leading to thrombus dissolution and activating a number of matrix metalloproteinases
-
-
?
pro-hepatic growth factor + H2O
mature hepatic growth factor + ?
-
uPA activates the hepatic growth factor from its inactive single-chain form to the active alpha-chain form
-
-
?
pro-hepatic growth factor + H2O
mature hepatic growth factor + ?
-
uPA activates the hepatic growth factor from its inactive single-chain form to the active alpha-chain form
-
-
?
S-2444 + H2O
pyroGlu-Gly-Arg + 4-nitroaniline
-
i.e. pyro-Glu-Gly-Arg-p-nitroanilide, a chromogenic substrate
-
-
?
urokinase plasminogen activator receptor + H2O
?
-
receptor cleavage by u-PA, u-PAR is susceptible to proteolysis by its cognate ligand and several other proteases, biological significance, overview
-
-
?
urokinase plasminogen activator receptor + H2O
?
-
receptor cleavage by u-PA, u-PAR is susceptible to proteolysis by its cognate ligand and several other proteases
-
-
?
additional information
?
-
-
binding of single-chain uPA moiety to its substrate plasminogen occurs with lower affinity compared to binding of the two-chain uPA moiety
-
-
-
additional information
?
-
-
disulfide bridges in the catalytic domain are essential for maintaining amidolytic and fibrinolytic activity
-
-
-
additional information
?
-
-
the enzyme cleaves its cellular receptor between domains 1 and 2
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator includes its single-chain zymogen, pro-urokinase and two-chain enzyme urokinase
-
?
additional information
?
-
-
active enzyme promotes tumor progression, activation of enzyme appears as a key step in tumor progression
-
-
-
additional information
?
-
-
enzyme released by alveolar epithelial cells alters alveolar epithelial repair in vitro by modulating the underlying fibrin matrix
-
-
-
additional information
?
-
-
structure and interdomain contacts of the N-terminal domain of the enzyme with the uPA receptor, binding structure, mechanisms responsible for the cellular responses induced by uPA binding, overview
-
-
-
additional information
?
-
-
the enzyme is a serine protease involved in tissue remodeling and cell migration, the active form of uPA is bound to its high affinity receptor on the cell surface, where specific inhibitors modulate its enzymatic activity, such inhibitors also regulate the cell surface levels of uPA by triggering the internalization of the uPA-receptor-inhibitor complex via endocytosis, overview, the C-terminus of the N-terminal region contains a sequence that interacts with alphaVbeta3 integrin and is relevant for cell migration, overview
-
-
-
additional information
?
-
-
the enzyme is involved in colorectal cancer invasion and metastasis
-
-
-
additional information
?
-
-
the enzyme plays a major role in extracellular proteolytic events associated with tumor cell growth, migration and angiogenesis
-
-
-
additional information
?
-
-
the enzyme-plasminogen activator inhibitor-1 complex in intenalized by endocytosis via binding of membrane-bound receptors, overview
-
-
-
additional information
?
-
-
trans-3,4-dimethyl-3-hydroxyflavanone, a hair growth enhancing active component, decreases active transforming growth factor beta2 and the TGF-b 2 activation cascade through control of uPA on the surface of keratinocytes, mechanism, overview
-
-
-
additional information
?
-
-
uPA interacts with the uPA receptor, which is important for many of the enzyme's biological functions
-
-
-
additional information
?
-
-
the amino-terminal fragment ATF of uPA contains an EGF-like and a kringle domain, involved in the binding of the receptor, chain B contains the catalytic site and maintains the ability to activate plasminogen also when it is not bound to the receptor, the C-terminus of the N-terminal region contains a sequence that interacts with alphaVbeta3 integrin and is relevant for cell migration, overview
-
-
-
additional information
?
-
-
incubation of THP-1 macrophage-like cells with uPA results in increased expression of paraoxonase 2. The effect requires uPA/uPA receptor interaction and is abolished by cell treatment with antioxidants. Presence of uPA increases macrophage oxidative stress, reactive oxygen formation, superoxide anion release, and cell-mediated low-density lipoprotein oxidation. Effects are related to uPA-mediated activation of NADPH oxidase
-
-
-
additional information
?
-
-
uterine natural killer cells may regulate extravillous trophoblast invasion and spiral artery remodeling via the uPA system
-
-
-
additional information
?
-
-
uPA and uPAderived peptides maintaining an amino-terminal fragment growth factor-like domain, including the so-called Omega loop, but not the enzymatically competent low molecular weight fragment, inhibit HIV expression in chronically infected U1 cells stimulated with either phorbol 12-myristate 13-acetate or tumor necrosis factor alpha. Both uPA receptor siRNA ands soluble anti-beta1/beta2 monomclonal antibodies abolish the anti-HIV effects of uPA
-
-
-
additional information
?
-
-
uPA forms a complex with its cogante receptor uPAR, specific interctions, analysis, overview
-
-
-
additional information
?
-
-
uPA, uPA receptor, and plasminogen activator inhibitor form the urokinase-type plasminogen activator system
-
-
-
additional information
?
-
-
uPA-uPAR complexes concentrate the plasmin production that provides extracellular matrix proteolysis, weakened cell-cell contact, and increased cell motility. The proteolytic mechanisms include uPA-induced plasmin generation at focal adhesion sites, which results in extracellular matrix degradation and thus facilitates the detachment of the cell's trailing edge. Plasmin inhibitors can suppress cell migration both in vitro, mechanisms by which uPA can regulate arterial remodeling, angiogenesis, and cell migration and proliferation after arterial injury, overview. Urokinase signaling, overview
-
-
-
additional information
?
-
-
urokinase-type plasmin activator, uPA, binding to uPA receptor, uPAR, induces migration/invasion through multiple interactors including integrins, overview. ECRG2 binds specifically to the kringle domain of uPA, and forms a complex with uPA-uPAR, the trinary complex modifies the dynamical association of uPAR with beta1 integrins. Identification of ECRG2-binding sequence in uPA, overview. Complex disruption inhibits the Src/mitogen-activated protein kinase pathway, resulting in suppression of cell migration/invasion
-
-
-
additional information
?
-
-
uPA-induced phosphorylation of endothelial nitric oxide synthase, eNOS, which is inhibited by myristoylated PKI, a protein kinase A inhibitor
-
-
-
additional information
?
-
-
no activity with the epithelial sodium channel alpha subunit, the enzyme shows amidolytic activity with fluorogenic substrate Pefafluor uPA
-
-
-
additional information
?
-
-
enzyme protein is consistently elevated in the hyperproliferative hair follicle keratinocyte, and inhibiton of enzyme decreases hair follicle keratinocyte proliferation
-
-
-
additional information
?
-
-
the enzyme supports liver repair independent of its cellular receptor uPAR, overview
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator and macrophages are required for skeletal muscle hypertrophy in mice, depletion of macrophages leads to reduced hypertrophy of muscles, overview
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator plays essential roles in skeletal muscle regeneration and healing, macrophage depletion leads to impaired muscle regeneration, molecular mechanism, overview, the macrophage enzyme is essentially required for chemotaxis, mechanism independent of receptor binding, overview
-
-
-
additional information
?
-
-
recombinant uPA binds purified soluble human integrin alphanybeta3, overview
-
-
-
additional information
?
-
-
addition of uPA to natural killer cell receptor Ly49E positive adult and fetal natural killer cells inhibits interferon-gamma secretion and reduces their cytotoxic potential, respectively. Effects are dependent on receptor Ly49E
-
-
-
additional information
?
-
-
incubation of macrophages with uPA results in increased expression of paraoxonase 2. The resulting effects such as increase in macrophage oxidative stress, reactive oxygen formation, superoxide anion release, and cell-mediated low-density lipoprotein oxidation cannot be reproduced in macrophages harvested from p47phox-/- mice
-
-
-
additional information
?
-
-
induction of endotoxin lipopolysaccharide-mediated uPA receptor expression is mediated through tyrosine phosphorylation of phophoglycerate kinase and heterogenous nuclear ribonucleoprotein C. This involves expression of uPA as an obligate intermediary
-
-
-
additional information
?
-
-
inhalation of urokinase-type plasminogen activator reduces airway remodeling in a murine asthma model, overview. The uPA/plasmin system participates in pericellular proteolysis and is capable of directly degrading matrix components, activating latent proteinases, and activating growth factors
-
-
-
additional information
?
-
-
uPA-uPAR complexes concentrate the plasmin production that provides extracellular matrix proteolysis, weakened cell-cell contact, and increased cell motility. The proteolytic mechanisms include uPA-induced plasmin generation at focal adhesion sites, which results in extracellular matrix degradation and thus facilitates the detachment of the cell's trailing edge. Plasmin inhibitors can suppress cell migration both in vitro, mechanisms by which uPA can regulate arterial remodeling, angiogenesis, and cell migration and proliferation after arterial injury, overview. Urokinase signaling, overview
-
-
-
additional information
?
-
-
inhalation of urokinase-type plasminogen activator reduces airway remodeling in a murine asthma model, overview. The uPA/plasmin system participates in pericellular proteolysis and is capable of directly degrading matrix components, activating latent proteinases, and activating growth factors
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator and macrophages are required for skeletal muscle hypertrophy in mice, depletion of macrophages leads to reduced hypertrophy of muscles, overview
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator plays essential roles in skeletal muscle regeneration and healing, macrophage depletion leads to impaired muscle regeneration, molecular mechanism, overview, the macrophage enzyme is essentially required for chemotaxis, mechanism independent of receptor binding, overview
-
-
-
additional information
?
-
-
lyses fibrin clots containing plasminogen but not plasminogen-free fibrin
-
-
-
additional information
?
-
-
uPA-uPAR complexes concentrate the plasmin production that provides extracellular matrix proteolysis, weakened cell-cell contact, and increased cell motility. The proteolytic mechanisms include uPA-induced plasmin generation at focal adhesion sites, which results in extracellular matrix degradation and thus facilitates the detachment of the cell's trailing edge. Plasmin inhibitors can suppress cell migration both in vitro, mechanisms by which uPA can regulate arterial remodeling, angiogenesis, and cell migration and proliferation after arterial injury, overview. Urokinase signaling, overview
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
alpha6 integrin + H2O
?
-
alpha6 integrin is present on prostate carcinoma escaping the gland via nerves. Urokinase-dependent cleavage of the laminin binding domain from the prostate tumor cell surface
-
-
?
urokinase plasminogen activator receptor + H2O
?
-
receptor cleavage by u-PA, u-PAR is susceptible to proteolysis by its cognate ligand and several other proteases, biological significance, overview
-
-
?
plasminogen + H2O
?
-
the enzyme mediates pericellular proteolysis during cell migration and tissue remodelling under physiological and pathophysiological conditions
-
-
-
plasminogen + H2O
?
-
potential role for uPA is a direct regulation of metalloproteinases-mediated extracellular proteolysis via the cleavage of the 72000 MW gelatinase/type IV collagenase to an 62000 MW form
-
-
-
plasminogen + H2O
?
-
key enzyme in the thrombolytic cascade converting plasminogen into plasmin, which in turn degrades thrombus fibrin
-
-
-
plasminogen + H2O
?
-
the enzyme promotes fibrinolysis by catalyzing the conversion of plasminogen to plasmin
-
-
-
plasminogen + H2O
?
-
when localized to the external cell surface it contributes to tissue remodelling and cellular migration
-
-
-
plasminogen + H2O
?
-
the enzyme is responsible for plasminogen activation, it is also involved in cell adhesion, chemotaxis, and proliferation, the signaling events are not mediated by uPA receptor uPAR/CD87, but require the kringle domain of the enzyme, which binds integrin alphanybeta3 for induction of cell migration, e.g. of CHO cells, overview
-
-
?
plasminogen + H2O
plasmin + ?
-
-
669677, 683130, 683220, 683299, 683456, 683550, 707518, 707866, 707901, 708639, 710248, 717213, 717386, 717916, 718142, 731365, 731429, 732801
-
-
?
plasminogen + H2O
plasmin + ?
-
principal function is fibrinolysis, u-PA also been implicated in other physiological functions such as embryogenesis, cell migration, tissue remodeling, ovulation, and wound healing
-
?
plasminogen + H2O
plasmin + ?
-
hearts with end-stage failure and fibrosis have macrophage accumulation and elevated plasminogen activator activity, mechanisms that link macrophage accumulation and plasminogen activator activity with cardiac fibrosis, dependent on localization of uPA by the uPA receptor uPAR, on activation of plasminogen by uPA and subsequent activation of transforming growth factor-beta1 and matrix metalloproteinase MMP-2 and MMP-9 by plasmin, overview, uPA-induced cardiac fibrosis can be attenuated by treatment with verapamil, plasminogen is necessary for uPA-induced cardiac fibrosis and macrophage accumulation, but uPAR is not
-
-
?
plasminogen + H2O
plasmin + ?
-
the uPA proteolytic domain specifically cleaves plasminogen and converts it into the serine protease plasmin with wide substrate specificity. Plasmin directly degrades fibrin, leading to thrombus dissolution and activating a number of matrix metalloproteinases
-
-
?
plasminogen + H2O
plasmin + ?
-
u-PA forms a complex with its receptor u-PAR in plasminogen ativation
-
-
?
plasminogen + H2O
plasmin + ?
-
the urokinase-type and tissue-type plasminogen activators regulate liver matrix remodelling through the conversion of plasminogen to the active protease plasmin, uPA is bound to its receptor uPAR, overview
-
-
?
plasminogen + H2O
plasmin + ?
-
the uPA proteolytic domain specifically cleaves plasminogen and converts it into the serine protease plasmin with wide substrate specificity. Plasmin directly degrades fibrin, leading to thrombus dissolution and activating a number of matrix metalloproteinases
-
-
?
plasminogen + H2O
plasmin + ?
-
the uPA proteolytic domain specifically cleaves plasminogen and converts it into the serine protease plasmin with wide substrate specificity. Plasmin directly degrades fibrin, leading to thrombus dissolution and activating a number of matrix metalloproteinases
-
-
?
pro-hepatic growth factor + H2O
mature hepatic growth factor + ?
-
uPA activates the hepatic growth factor from its inactive single-chain form to the active alpha-chain form
-
-
?
pro-hepatic growth factor + H2O
mature hepatic growth factor + ?
-
uPA activates the hepatic growth factor from its inactive single-chain form to the active alpha-chain form
-
-
?
additional information
?
-
-
active enzyme promotes tumor progression, activation of enzyme appears as a key step in tumor progression
-
-
-
additional information
?
-
-
enzyme released by alveolar epithelial cells alters alveolar epithelial repair in vitro by modulating the underlying fibrin matrix
-
-
-
additional information
?
-
-
structure and interdomain contacts of the N-terminal domain of the enzyme with the uPA receptor, binding structure, mechanisms responsible for the cellular responses induced by uPA binding, overview
-
-
-
additional information
?
-
-
the enzyme is a serine protease involved in tissue remodeling and cell migration, the active form of uPA is bound to its high affinity receptor on the cell surface, where specific inhibitors modulate its enzymatic activity, such inhibitors also regulate the cell surface levels of uPA by triggering the internalization of the uPA-receptor-inhibitor complex via endocytosis, overview, the C-terminus of the N-terminal region contains a sequence that interacts with alphaVbeta3 integrin and is relevant for cell migration, overview
-
-
-
additional information
?
-
-
the enzyme is involved in colorectal cancer invasion and metastasis
-
-
-
additional information
?
-
-
the enzyme plays a major role in extracellular proteolytic events associated with tumor cell growth, migration and angiogenesis
-
-
-
additional information
?
-
-
the enzyme-plasminogen activator inhibitor-1 complex in intenalized by endocytosis via binding of membrane-bound receptors, overview
-
-
-
additional information
?
-
-
trans-3,4-dimethyl-3-hydroxyflavanone, a hair growth enhancing active component, decreases active transforming growth factor beta2 and the TGF-b 2 activation cascade through control of uPA on the surface of keratinocytes, mechanism, overview
-
-
-
additional information
?
-
-
uPA interacts with the uPA receptor, which is important for many of the enzyme's biological functions
-
-
-
additional information
?
-
-
incubation of THP-1 macrophage-like cells with uPA results in increased expression of paraoxonase 2. The effect requires uPA/uPA receptor interaction and is abolished by cell treatment with antioxidants. Presence of uPA increases macrophage oxidative stress, reactive oxygen formation, superoxide anion release, and cell-mediated low-density lipoprotein oxidation. Effects are related to uPA-mediated activation of NADPH oxidase
-
-
-
additional information
?
-
-
uterine natural killer cells may regulate extravillous trophoblast invasion and spiral artery remodeling via the uPA system
-
-
-
additional information
?
-
-
uPA forms a complex with its cogante receptor uPAR, specific interctions, analysis, overview
-
-
-
additional information
?
-
-
uPA, uPA receptor, and plasminogen activator inhibitor form the urokinase-type plasminogen activator system
-
-
-
additional information
?
-
-
uPA-uPAR complexes concentrate the plasmin production that provides extracellular matrix proteolysis, weakened cell-cell contact, and increased cell motility. The proteolytic mechanisms include uPA-induced plasmin generation at focal adhesion sites, which results in extracellular matrix degradation and thus facilitates the detachment of the cell's trailing edge. Plasmin inhibitors can suppress cell migration both in vitro, mechanisms by which uPA can regulate arterial remodeling, angiogenesis, and cell migration and proliferation after arterial injury, overview. Urokinase signaling, overview
-
-
-
additional information
?
-
-
urokinase-type plasmin activator, uPA, binding to uPA receptor, uPAR, induces migration/invasion through multiple interactors including integrins, overview. ECRG2 binds specifically to the kringle domain of uPA, and forms a complex with uPA-uPAR, the trinary complex modifies the dynamical association of uPAR with beta1 integrins. Identification of ECRG2-binding sequence in uPA, overview. Complex disruption inhibits the Src/mitogen-activated protein kinase pathway, resulting in suppression of cell migration/invasion
-
-
-
additional information
?
-
-
uPA-induced phosphorylation of endothelial nitric oxide synthase, eNOS, which is inhibited by myristoylated PKI, a protein kinase A inhibitor
-
-
-
additional information
?
-
-
enzyme protein is consistently elevated in the hyperproliferative hair follicle keratinocyte, and inhibiton of enzyme decreases hair follicle keratinocyte proliferation
-
-
-
additional information
?
-
-
the enzyme supports liver repair independent of its cellular receptor uPAR, overview
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator and macrophages are required for skeletal muscle hypertrophy in mice, depletion of macrophages leads to reduced hypertrophy of muscles, overview
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator plays essential roles in skeletal muscle regeneration and healing, macrophage depletion leads to impaired muscle regeneration, molecular mechanism, overview, the macrophage enzyme is essentially required for chemotaxis, mechanism independent of receptor binding, overview
-
-
-
additional information
?
-
-
addition of uPA to natural killer cell receptor Ly49E positive adult and fetal natural killer cells inhibits interferon-gamma secretion and reduces their cytotoxic potential, respectively. Effects are dependent on receptor Ly49E
-
-
-
additional information
?
-
-
incubation of macrophages with uPA results in increased expression of paraoxonase 2. The resulting effects such as increase in macrophage oxidative stress, reactive oxygen formation, superoxide anion release, and cell-mediated low-density lipoprotein oxidation cannot be reproduced in macrophages harvested from p47phox-/- mice
-
-
-
additional information
?
-
-
induction of endotoxin lipopolysaccharide-mediated uPA receptor expression is mediated through tyrosine phosphorylation of phophoglycerate kinase and heterogenous nuclear ribonucleoprotein C. This involves expression of uPA as an obligate intermediary
-
-
-
additional information
?
-
-
inhalation of urokinase-type plasminogen activator reduces airway remodeling in a murine asthma model, overview. The uPA/plasmin system participates in pericellular proteolysis and is capable of directly degrading matrix components, activating latent proteinases, and activating growth factors
-
-
-
additional information
?
-
-
uPA-uPAR complexes concentrate the plasmin production that provides extracellular matrix proteolysis, weakened cell-cell contact, and increased cell motility. The proteolytic mechanisms include uPA-induced plasmin generation at focal adhesion sites, which results in extracellular matrix degradation and thus facilitates the detachment of the cell's trailing edge. Plasmin inhibitors can suppress cell migration both in vitro, mechanisms by which uPA can regulate arterial remodeling, angiogenesis, and cell migration and proliferation after arterial injury, overview. Urokinase signaling, overview
-
-
-
additional information
?
-
-
inhalation of urokinase-type plasminogen activator reduces airway remodeling in a murine asthma model, overview. The uPA/plasmin system participates in pericellular proteolysis and is capable of directly degrading matrix components, activating latent proteinases, and activating growth factors
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator and macrophages are required for skeletal muscle hypertrophy in mice, depletion of macrophages leads to reduced hypertrophy of muscles, overview
-
-
-
additional information
?
-
-
urokinase-type plasminogen activator plays essential roles in skeletal muscle regeneration and healing, macrophage depletion leads to impaired muscle regeneration, molecular mechanism, overview, the macrophage enzyme is essentially required for chemotaxis, mechanism independent of receptor binding, overview
-
-
-
additional information
?
-
-
uPA-uPAR complexes concentrate the plasmin production that provides extracellular matrix proteolysis, weakened cell-cell contact, and increased cell motility. The proteolytic mechanisms include uPA-induced plasmin generation at focal adhesion sites, which results in extracellular matrix degradation and thus facilitates the detachment of the cell's trailing edge. Plasmin inhibitors can suppress cell migration both in vitro, mechanisms by which uPA can regulate arterial remodeling, angiogenesis, and cell migration and proliferation after arterial injury, overview. Urokinase signaling, overview
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-
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1-[(N-benzylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
1-[3'-([3,5-difluoro-6-[5-methyl-2-(1H-tetrazol-1-yl)phenoxy]pyridin-2-yl]oxy)biphenyl-3-yl]methanamine
-
-
2-(4-chloro-7-(2-cyano-6-methoxyphenyl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(4-chloro-7-(2-methoxyphenyl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(4-chloro-7-(3-methoxyphenyl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(7-(1,3-benzodioxol-5-yl)-4-chloroisoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(7-(1,3-benzodioxol-5-yl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(7-phenylisoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
-
-
2-phenethyl-SO2-D-Ser-Ala-Arg-al
-
is an irreversible urokinase inhibitor, and an alkylating agent forming a covalent adduct with an active site of the enzyme
2-[(6-[[3',5-bis(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)-5-hydroxybiphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-3-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(propan-2-yl)benzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methoxybenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-nitrobenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-5-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-6-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[[2-(dimethylamino)ethyl](methyl)amino]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
-
-
2-[(6-[[4'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
-
-
2-[(6-[[4-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[6-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[2-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
-
2-[2-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
-
2-[3-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)propyl]isothiourea hydrobromide
-
-
2-[3-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy]propyl)isothiourea hydrobromide
-
-
2-[[3,5-difluoro-6-([3'-[(methylamino)methyl]biphenyl-3-yl]oxy)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(methylamino)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(morpholin-4-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(piperazin-1-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-(dimethylamino)-3,5-difluoropyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide
-
i.e. amiloride, selectively inhibits the enzyme, but not tissue plasminogen activator or other serine protease members of the trypsin superfamily
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)-5-methoxybenzoic acid
-
comparison of selectivity with t-plasminogen activator and plasmin
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
comparison of selectivity with t-plasminogen activator and plasmin
3-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
-
-
3-[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]propanoic acid
-
-
4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxamide
-
slight inhibition
4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide
-
inhibitor with moderate clearance level, high volume of distribution, and long half-life of 7.5 hours. More than 50 fold selective for uPA over all but one of the enzymes tested. Selectivity against trypsin is only 3- to 4fold
4-(2-aminoethoxy)-N-[3-chloro-2-ethoxy-5-(piperidin-1-yl)phenyl]-3,5-dimethylbenzamide
-
-
4-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
comparison of selectivity with t-plasminogen activator and plasmin
4-(dimethylamino)-2-[[6-([3'-[(dimethylamino)methyl]biphenyl-3-yl]oxy)-3,5-difluoropyridin-2-yl]oxy]benzoic acid
-
-
4-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
-
-
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
-
-
7-methoxy-8-[1-(methylsulfonyl)-1H-pyrazol-4-yl]naphthalene-2-carboximidamide
-
-
antibody DS2
-
isolation and affinity maturation of a fully human recombinant antibody, that is specific to the human uPA and capable of inhibiting its enzymatic activity with an IC50 value in the low nanomolar range, overview. Ability of the DS2 antibody to preferentially localize at the tumor site compared with healthy organs
-
antibody mU3
-
binding of mU3 to the 37- and 70-loops, the antibody stabilizes the active conformation of the enzyme, the N-terminus (Ile16) of the truncated enzyme muPA(16-243) is less exposed upon binding of mU3
-
bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
-
di-(4-acetamidophenyl) 1-[(N-benzyloxycarbonyl-D-seryl)-Lalanyl]amino-2-[4-(guanidino)phenyl]-ethanephosphonate trifluoroacetate
-
-
diphenyl (N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(3-guanylpropyl)methanephosphonate
-
50% inhibition at 0.000061 mM
diphenyl (N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(4-guanylbutyl)methanephosphonate
-
50% inhibition at 0.00025 mM
diphenyl (N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(4-guanylphenyl)methanephosphonate
-
50% inhibition at 0.0016 mM
diphenyl 1-(N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-2-(4-guanylphenyl)ethanephosphonate
-
50% inhibition at 0.000057 mM
diphenyl 1-[(N-2-acetoadamantanyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-2-acetothiophenyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-benzenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-benzoyloxycarbonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-benzoylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-naphtalenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-o,o-dimethylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-o-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-bromobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-cyanobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-methoxybenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N2-thiophenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
-
enzyme-specific antibody
-
significant reduction of hair follicle keratinocyte proliferation
-
ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate
-
-
i-Boc-D-Ser-Ala-Arg-al
-
is an alkylating agent, and irreversibly inhibits urokinase by forming a covalent adduct with an active site of the enzyme
maspin
-
regulates uPA-dependent processes in vivo not involving its RCL sequence with Arg340, but is inable to directly inhibit uPA catalytic activity in vitro, binds the enzyme in both singlechain and double-chain forms, maspin is a member of the serpin family with a reactive center loop that is incompatible with proteinase inhibition by the serpin conformational change mechanism, overview
meloxicam
-
reduces enzyme secretion in chondral and synovial cultures downregulating the PA/plasmin system
methylprednisolone
-
reduces enzyme secretion in chondral and synovial cultures downregulating the PA/plasmin system
monoclonal antibody mU1
-
murine monoclonal antibody directed against murine uPA. mU1 blocks uPA-catalyzed plasminogen activation in vitro, as well as plasmin-mediated pro-uPA activation. Systemic administration of mU1 rescues mice treated with a uPA-activable anthrax protoxi and impairs uPA-mediated hepatic fibrinolysis in tissue-type plasminogen activator-deficient mice, resulting in a phenotype mimicking that of uPA/tPA double deficient mice
-
mupain-1-16
-
the inhibitor stabilizes the active conformation of the enzyme, the N-terminus (Ile16) of the truncated enzyme muPA(16-243) is less exposed upon binding of mupain-1-16
N-(3'-chlorobiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
slight inhibition
N-(3'-fluorobiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
slight inhibition
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-prolinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-aminobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-methylbenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-nitrobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[3-(3-bromopropoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide
-
competitive reversible inhibition mechanism, the bromine occupies the same position as positively charged arginino mimetic groups, molecular modeling
N-[4-(aminomethyl)phenyl]-6-carbamimidoyl-4-(pyrimidin-2-ylamino)naphthalene-2-carboxamide
-
-
N-[[4-(methoxycarbonyl)benzyl]sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
comparison of specificity with five additional trypsin-like serine-proteases
naproxen
-
reduces enzyme secretion in chondral and synovial cultures downregulating the PA/plasmin system
PA inhibitor type 1
-
PAI-1, effects of uPA-PAI-1 are abrogated by the nitric-oxide synthase inhibitor N-D-nitro-L-arginine methyl ester. Dramatically elevated levels in case of acute lung injury
-
PAI-2
-
i.e. plasminogen activator inhibitor type 2, cell-surface enzyme:PAI-2 complex formation is reflective of complete enzyme inhibition, kinetic analysis of inhibition
-
PD 098059
-
hepatocyte growth factor-mediated uPA secretion by Hep-G2 cells is reduced with increasing concentrations of PD 098059
PD98059
-
the ERK MAP kinase inhibitor dramatically reduces the uPA expression in the frozen-thawed porcine uterus endometrial epithelium cells
Plumbagin
-
leads to uPA inhibition and downregulation, inhibits adhesion, migration and invasion in HepG2 cells
staphylokinase
-
competitively inhibits plasminogen activation by endogenous uPA. The N-terminal residues of staphylokinase are important for inhibition
-
trans-3,4'-dimethyl-3-hydroxyflavanone
-
i.e. t-flavanone, a synthetic compound with hair growth enhancing activity that is effective against male pattern alopecia, inhibits the enzyme on the surface of keratinocytes, overview
trans-diphenyl N-(N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(4-(guanylmethyl)-cyclohexyl)methanephosphonate
-
50% inhibition at 0.0011 mM
TX-1877
-
hypoxic cell radiosensitizer. Treatment of nude mice bearing subcutaneously or orthotopically implanted human colon cancer cell lines HCT-116 and HT-29 with TX-1877, irradiation or TX-1877 with irradiation results in significant inhibition of matrix metalloproteinase-9 and uPA. Treatments also inhibit the para-aortic lymph node metastasis, however, do not prolong the survival in orthotopic model. In the subcutaneous model, tumors treated with TX-1877 and irradiation show significant reductions in volume
[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]acetic acid
-
-
ecotin
-
inhibits uPA almost 10000-fold less efficiently than trypsin, ecotin is expressed on the surface of filamentous bacteriophage, each of the selected ecotin variants (M84R, M84K, M84R/M85R and M84R/M85K) exhibits increased affinity for uPA when compared to wild-type ecotin, with ecotin M84R/M85R showing 2800-fold increase in binding affinity
-
mupain-1
-
i.e. CPAYSRYLDC, isolated from a murine peptide library and reconstructed, no inhibition of wild-type human enzyme, since the inhibitor is highly specific for the murine enzyme, but inhibition by the human enzyme mutant H99Y, overview, expression of mupain-1 peptide sequence in fusion with the N-terminal domains of the phage coat protein g3p in Escherichia coli
mupain-1
-
i.e. CPAYSRYLDC, isolated from a murine peptide library and reconstructed, competitive and highly selective inhibitor, R6 of mupain-1 is the P1 residue, extended binding interaction including the P5, P3, P2, P1, and P1' residues of mupain-1 and the specificity pocket, the catalytic triad, and the amino acids 41, 99 and 192 located in and around the active site of murine uPA, overview, expression of mupain-1 peptide sequence in fusion with the two N-terminal domains of g3p, D1 and D2 in Escherichia coli
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
comparison of specificity with five additional trypsin-like serine-proteases
PAI-1
-
a proteolytic inhibitor of uPA, blocks the increase in proliferation of myoblasts induced by uPA
-
plasminogen activator inhibitor 1
-
phosphorylated uPA is less sensitive to inhibition than nonphosphorylated uPA
plasminogen activator inhibitor 1
-
binding of single-chain uPA moiety to the inhibitor occurs with lower affinity compared to binding of the two-chain uPA moiety
plasminogen activator inhibitor 1
-
phosphorylated enzyme is inhibited 50% at a concentration 4fold higher than nonphosphorylated enzyme
plasminogen activator inhibitor 1
-
PAI-1, complete inhibition, elevated inhibitor specifically inactivates pulmonary urokinase-type plasminogen activator and tissue.type plasminogen activator, EC 3.4.21.68
plasminogen activator inhibitor type-1
-
i.e. PAI type-1, the endogenous inhibitor expression is higher in myometrium than in myoma in the uterus myomatosus, overview
-
plasminogen activator inhibitor type-1
-
i.e. PAI-1, an endogenous inhibitor protein
-
plasminogen activator inhibitor-1
-
i.e. PAI-1, complexes the enzyme, binding structure, the 10-100-fold higher affinity of the uPA-PAI-1 complex compared with the free components depends on the bonus effect of bringing the binding areas on uPA and PAI-1 together on the same binding entity, overview, inhibitor mutants K71A/R78A/Y81A/K82A, K82A-R120A, and R78A-K124A show reduced binding to the enzyme and the enzyme receptors, effects of several mutations of the inhibitor protein on complex formation and endocytosis, overview
plasminogen activator inhibitor-1
-
i.e. PAI-1, recombinantly expressed with an N-terminal His6-tag and purified from Escherichia coli cells, labeled with N,N0-dimethyl-N-(iodoacetyl)-N0-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)ethylenediamine, i.e. P9-NBD-labeled PAI-1. Slow formation of a covalent serpin-protease complex between single-chain uPA and PAI-1 is significantly accelerated in the presence of specific dipeptide sequences
plasminogen activator inhibitor-1
-
PAI-1, specifically and rapidly inhibits urokinase-type plasminogen activator uPA and tissue-type plasminogen activator, tPA, EC 3.4.21.68. The PAI-1 reactive center loop serves as a bait to attract uPA onto the top of the PAI-1 molecule. P4–P3' residues of the reactive center loop interact extensively with the uPA catalytic site, accounting for about two-thirds of the total contact area, also almost all uPA exosite loops, including the 37-, 60-, 97-, 147-, and 217-loops, are involved in the interaction with PAI-1, of the residues of the 37-loop, Arg-E37a plays the most important role, Michaelis complex formation, overview. The recombinant stable His-tagged PAI-1 mutant 14-1B containing four point mutations N150H, K154T, Q319L, and M354I, is expressed in Escherichia coli strain C41(DE3) using the expression vector pT7-PL
additional information
-
humanized murine ATF, i.e. an amino-terminal fragment of urokinase, represses 79% of membrane-associated enzyme activity on MDA-MB-231 cells, murine ATF represses 29% of activity
-
additional information
-
development of potent uncharged inhibitors of uPA based upon the isocoumarin scaffold, bromine occupies the same position as positively charged arginino mimetic groups, structure activity relationships, inhibitor synthesis and molecular modeling, overview
-
additional information
-
the active form of uPA is bound to its high affinity receptor on the cell surface, where specific inhibitors modulate its enzymatic activity, such inhibitors also regulate the cell surface levels of uPA by triggering the internalization of the uPA-receptor-inhibitor complex via endocytosis
-
additional information
-
quantitative structure-activity relationship analysis of substituted 2-pyridinyl guanidines as selective inhibitors using QuaSAR descriptors of molecular modeling software MOE. uPA inhibitory activity of core-substitued 2-pyridinyl guanidines is influenced by their molecular shape, molecular flexibility and halogen atoms in the molecule. uPA inhibitory activity of 2-(5-chloropyridin-2-yl) guanidines with bulky substituents in position 3 is dependent on molecular lipophilicity, number of double bonds and spatial orientation of bulky substituents in the molecule
-
additional information
-
stable expression of dominant-negative MEK-1 in Hep-G2 cells decreases S hepatocyte growth factor-mediated uPA secretion
-
additional information
-
identification of potent, selective, and orally bioavailable non-amidine uPA inhibitors, binding in the S1 pocket, overview
-
additional information
-
Thrombin hydrolysis provides the mechanism of proteolytic inactivation of uPA cleavage of the Arg156-Phe157 enzyme bond that does not exclude nonproteolytic functioning of such peptide forms
-
additional information
-
synthesis of peptides competing with uPA for binding to the specific uPA receptor, usage of the SAAC methodology to regioselectively label the peptides, overview
-
additional information
-
the autolysis loop in the catalytic domain of uPA is a potential inhibitory target. Three antibodies are potent inhibitors of uPA activity, two pro-uPA-specific ones by inhibiting conversion of pro-uPA to active uPA and an active uPA-specific antibody by shielding the access of plasminogen to the active site, overview. The conformation-specific antibodies mAb-112 and mAb-12E6B10 are useful to selectively stain pro-uPA or active uPA on the surface of cultured cells. Antibody mAb-112 is a non-competitive inhibitor of S-2444 cleavage by uPA with a Ki similar to the Kd for mAb-112 binding to active two-chain uPA. The epitopes of the conformation-specific antibodies are all localized to the activation and/or autolysis loop, binding kinetic analysis and models of the three-dimensional structures, overview
-
additional information
-
efficacy of grape seed extract in negatively regulating uPA expression and cell migration using highly metastatic androgen-independent PC3 prostate cancer cells as a model. Grape seed extract inhibits and downregulates NFkB-dependent urokinase plasminogen activator promoter activity
-
additional information
-
synthesis and inhibitory potencies of d-Ser-Ala-Arg-NH-X peptides, overview. All compounds with a hydroxyl residue of an amide group do not inhibit urokinase, no inhibition by D-Ser-Ala-Arg-NH
-
additional information
-
2-amidino analogues of glycine-amiloride conjugates as inhibitors of urokinase-type plasminogen activator, design and synthesis, overview. Substitution of C2-acylguanidine of C5-glycyl-amiloride with amidine and amidoxime groups, respectively. Importance of maintaining C5-hydrophobicity
-
additional information
-
synthesis and evaluation of a series of naphthamide and naphthalene sulfonamides as enzyme inhibitors containing non-basic groups as substitute for amidine or guanidine groups, overview
-
additional information
-
enzyme inhibitior screening, genetic algorithm-based quantitative structure-activity relationship analysis to select the best possible combination of pharmacophoric models and physicochemical descriptors that can explain bioactivity variation within the training inhibitors, overview. At least three binding modes are accessible to ligands within the enzyme binding pocket
-
additional information
-
extracts of tropical plants show enzyme inhibition activity, e.g. extracts from Croton lucidus, Erythroxylum aerolatum, Tabebuia heterophylla, Lantana camara, Cananga odorata, and Amyris elemifera. Extracts from leaves of Croton lucidus, a small shrub in the Euphorbiaceae family, typically growing in the limestone hills, coastal forests in the subtropical dry forest life zone in southwestern Puerto Rico, show presence of a strong enzyme inhibitory activity, comparison of extract from petroleum ether, chloroform, ethyl acetate and n-butanol, overview. The chloroform extract shows the highest inhibitory potency with 74% inhibition and an IC50 value of 0.00352 mg/ml. Analysis of the cytostatic activity of the extracts on PaCa-2 cells, highest cytotxic effct by choroform, lowest by n-butanol extract
-
additional information
-
humanized murine ATF, i.e. an amino-terminal fragment of urokinase, represses 29% of membrane-associated enzyme activity on LLC cells, murine ATF represses 74% of activity
-
additional information
-
phage-displayed peptide library screening for murine uPA-binding peptide sequences, overview
-
additional information
-
the MAP kinase inhibitors SP600125, a JNK inhibitor, and SB203580, a p38 inhibitor, do not inhibit uPA in frozen-thawed porcine uterus endometrial epithelium cells
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1,3,8-trihydroxy-6-methylanthraquinone
-
i.e. emodin, an active compound of aloe. Emodin increases the fibrinolytic activity of fibroblast cells in a dose-dependent manner, linked to increased uPA activity and uPA gene up-regulation. Emodin also induces up-regulation of uPA inhibitor PAI-1. Up-regulations are independent of emodin's effect on nuclear factor kappaB. The effect on the uPA system may be via generation of reactive oxygen species
Ile-Ile
-
an Ile-Ile or Ile-Val dipeptide can induce limited enzyme activity in the single-chain zymogen form of uPA or its K158A variant, which cannot be activated proteolytically
Ile-Val
-
an Ile-Ile or Ile-Val dipeptide can induce limited enzyme activity in the single-chain zymogen form of uPA or its K158A variant, which cannot be activated proteolytically
integrin alpha v beta3
-
binds specifically to the enzyme and is required for plasminogen activation, overview
-
interleukin beta
-
significantly induces uPA expression and activity via protein kinase Calpha-dependent JNK1/2 and NIK cascades. Induction is inhibited by pretreatment with the inhibitors of JNK1/2, SP600125, of protein kinase C, Ro31-8220 and Go6976, or of nuclear factor kappaB, helenalin, and by transfection with dominant negative mutants of protein kinase C alpha, NIK, and IKKbeta, and siRNAs of JNK1/2 and p65
-
phorbol 12-myristate 13-acetate
-
stimulation of dental pulp cells by tumor necrosis factor-alpha results in increased uPA activity. Tumor necrosis factor-alpha-induced PA release is enhanced in the presence of phorbol 12-myristate 13-acetate
SB 203580
-
pretreatment of Hep-G2 cells with SB 203580 increases hepatocyte growth factor-mediated uPA secretion by 50-60%
tumor necrosis factor-alpha
-
stimulation of dental pulp cells results in increased uPA activity. Tumor necrosis factor-alpha-induced PA release is enhanced in the presence of phorbol 12-myristate 13-acetate
-
additional information
-
pro-urokinase upregulates the expression of urokinase-type plasminogen activator in pulmonary arterial endothelial cells, but not the expression level of the uPA receptor
-
additional information
-
binding of uPA to uPA receptor increases the catalytic efficiency by enhancing its activation by plasmin or other enzymes. uPAR promotes the invasive migration of hair follicles synergizing in manner dependent and independent of uPA during human prenatal morphogenesis
-
additional information
-
the enzyme is initially synthesized as single-chain proenzyme with an activity that is many orders of magnitude lower than those of the mature enzyme. Proteolytic cleavage of an exposed loop liberates a new amino terminus that inserts into a hydrophobic pocket and forms a stabilizing salt bridge with a ubiquitously conserved aspartate residue, resulting in a conformational change organizing the mature oxyanion hole
-
additional information
-
u-PAR in binding to u-PA initiates plasminogen activation. A cleavage-resistant u-PAR, cr-u-PAR, exhibits accelerated internalization and resurfacing due to direct association with the endocytic receptor alpha2-macroglobulin receptor/low density lipoprotein receptor-related protein in the absence of the enzyme inhibitor complex of active u-PA and plasminogen activator inhibitor-1
-
additional information
-
uPA needs to be activated proteolytically. Sphingosine 1-phosphate receptor S1P1 overexpression in U-118 MG cells results in potent stimulation of uPA activity regardless of S1P treatment, expression of receptors S1P2 and S1P3 does not affect uPA activity
-
additional information
-
cytokeratin 8 ectoplasmic domain binding by a specific monoclonal antibody inhibits activation of plasminogen, the synthetic dodecapeptide corresponding to the epitope sequence, VKIALEVEIATY, binds uPA. The antibody increases adhesion of breast tumor cells to fibronectin
-
additional information
-
plasmin and urokinase-type plasminogen activator can activate each other through proteolytic cleavage
-
additional information
-
increased plasminogen activator activity in the lung by administering exogenous uPA or by using mice genetically deficient in the uPA inhibitor plasminogen activator inhibitor-1, PAI-1
-
additional information
-
uPA transcription and activity is only markedly increased during chronic neurodegeneration, not during acute intracerebral lipopolysaccharide-induced or acute kainate-induced neurodegeneration. Increase in total plasminogen activation with progression of prion disease is apparent in both soluble and membrane fractions
-
additional information
-
increase of uPA activity and expression by freezing/thawing process in porcine uterus endometrial epithelium cells
-
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.297
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
-
pH 8.8, phosphorylated uPA
0.392
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
-
pH 7.5, phosphorylated uPA
0.438
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
-
pH 8.8, nonphosphorylated uPA
0.608
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
-
pH 7.5, nonphosphorylated uPA
additional information
additional information
-
binding kinetics of enzyme with enzyme receptors VLDLR-I, SorLA, or LRP-1A , overview
-
additional information
additional information
-
kinetic effects of dipeptides on the catalytic activity of single-chain uPA and two-chain uPA toward the chromogenic substrate S-2444, overview
-
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0075
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
-
pH 8.8, nonphosphorylated uPA
0.0113
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
-
pH 7.5, nonphosphorylated uPA
0.32
S2444
-
pH 7.4, 25°C, mutant S303E, single-chain activator; pH 7.4, 25°C, wild-type, single-chain activator
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kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0039
2-(1-hydroxynaphthalen-2-yl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0019
2-(2,6-dihydroxyphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.00028
2-(2-hydroxy-3-bromo-5-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.00025
2-(2-hydroxy-3-bromophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.00055
2-(2-hydroxy-3-fluorophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0036
2-(2-hydroxy-3-methoxyphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.008
2-(2-hydroxy-3-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0009
2-(2-hydroxy-3-nitrophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.013
2-(2-hydroxy-4-diethylaminophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0036
2-(2-hydroxy-4-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0037
2-(2-hydroxy-5-bromophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0005
2-(2-hydroxy-5-chlorobiphenyl-3-yl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0028
2-(2-hydroxy-5-fluorophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0036
2-(2-hydroxy-5-methoxyphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0075
2-(2-hydroxy-5-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0033
2-(2-hydroxy-5-nitrophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.0004
2-(2-hydroxybiphenyl-3-yl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37°C
0.00002
2-[2-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
pH 8.8, 25°C
0.000084
2-[2-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
pH 8.8, 25°C
0.000038
2-[3-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)propyl]isothiourea hydrobromide
-
pH 8.8, 25°C
0.00001
2-[3-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy]propyl)isothiourea hydrobromide
-
pH 8.8, 25°C
0.000009
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)-5-methoxybenzoic acid
-
-
0.000037
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
-
0.000082
4-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
-
0.00063
7-methoxy-8-[1-(methylsulfonyl)-1H-pyrazol-4-yl]naphthalene-2-carboximidamide
-
pH 7.4, 37°C
0.00041
ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate
-
pH 8.8, 37°C
0.00004
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
-
pH 8.8, 37°C
0.018
N-[(4-aminobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
-
0.0076
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
-
0.023
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
-
0.01
N-[(4-methylbenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
-
0.024
N-[(4-nitrobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
-
0.0014
N-[3-(2-bromoethoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide
-
pH 8.8, 25°C
0.000034
N-[3-(3-bromopropoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide
-
pH 8.8, 25°C
0.0000006
N-[4-(aminomethyl)phenyl]-6-carbamimidoyl-4-(pyrimidin-2-ylamino)naphthalene-2-carboxamide
-
pH 7.4, 37°C
0.018
N-[[4-(methoxycarbonyl)benzyl]sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
-
0.0065
3-(1-carbamimidoylpiperidin-3-yl)-L-alanine
-
pH 7.4, 37°C, wild-type enzyme
0.219
3-(1-carbamimidoylpiperidin-3-yl)-L-alanine
-
pH 7.4, 37°C, enzyme mutant H99Y
0.00248
3-(1-carbamimidoylpiperidin-4-yl)-L-alanine
-
pH 7.4, 37°C, enzyme mutant H99Y
0.045
3-(1-carbamimidoylpiperidin-4-yl)-L-alanine
-
pH 7.4, 37°C, wild-type enzyme
0.0000077
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
pH 8.8, 37°C
0.000002
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
-
pH 7.4, 37°C, compound uPA-I5
0.000003
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
-
pH 7.4, 37°C, compound uPA-I6
0.000006
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
-
pH 7.4, 37°C, compound uPA-I3
0.000014
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
-
pH 7.4, 37°C, compound uPA-I4
0.000021
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
-
pH 7.4, 37°C, compound uPA-I1
0.000028
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
-
pH 7.4, 37°C, compound uPA-I2
additional information
additional information
-
kinetic effects of dipeptides on the inhibition of single-chain uPA and two-chain uPA, overview. Stopped-flow kinetics of P9-NBD-labeled PAI-1, 25°C, overview
-
additional information
additional information
-
inhibition kinetics of mupain variants, overview
-
additional information
additional information
-
inhibition kinetics of mupain variants, overview
-
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000035
1-[(N-benzylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.013
1-[3'-([3,5-difluoro-6-[5-methyl-2-(1H-tetrazol-1-yl)phenoxy]pyridin-2-yl]oxy)biphenyl-3-yl]methanamine
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000098
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
0.0027
2-[(6-[[3',5-bis(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000023
2-[(6-[[3'-(aminomethyl)-5-hydroxybiphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00054
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-3-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00068
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(propan-2-yl)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00022
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methoxybenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00024
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
0.0013
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-nitrobenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0035
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-5-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.026
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-6-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00084
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000025
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0001
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[[2-(dimethylamino)ethyl](methyl)amino]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.03
2-[(6-[[4'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000089
2-[(6-[[4-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000039
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
0.000015
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.03
2-[(6-[[6-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.03
2-[[3,5-difluoro-6-([3'-[(methylamino)methyl]biphenyl-3-yl]oxy)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00013
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(methylamino)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0009
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(morpholin-4-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000065
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(piperazin-1-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00053
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-(dimethylamino)-3,5-difluoropyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.02
3-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.03
3-[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]propanoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000072
4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide
Rattus norvegicus;
-
-
0.000072
4-(2-aminoethoxy)-N-[3-chloro-2-ethoxy-5-(piperidin-1-yl)phenyl]-3,5-dimethylbenzamide
Homo sapiens;
-
pH 8.8, 37°C
0.03
4-(dimethylamino)-2-[[6-([3'-[(dimethylamino)methyl]biphenyl-3-yl]oxy)-3,5-difluoropyridin-2-yl]oxy]benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.03
4-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0002
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
Homo sapiens;
-
pH 8.8, 37°C
0.0021
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)-2-naphthamide
Homo sapiens;
-
pH 8.8, 37°C
0.0041
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens;
-
pH 8.8, 37°C
0.019
6-methoxy-N-(3'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens;
-
pH 8.8, 37°C
0.0069
6-methoxy-N-(3'-nitrobiphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens;
-
pH 8.8, 37°C
0.023
6-methoxy-N-(4'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens;
-
pH 8.8, 37°C
0.0000034
bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
Homo sapiens;
-
pH 8.8, 37°C
0.0000067
di-(4-acetamidophenyl) 1-[(N-benzyloxycarbonyl-D-seryl)-Lalanyl]amino-2-[4-(guanidino)phenyl]-ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.000008
diphenyl 1-[(N-2-acetoadamantanyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000069
diphenyl 1-[(N-2-acetothiophenyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000026
diphenyl 1-[(N-benzenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000043
diphenyl 1-[(N-benzoyloxycarbonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.000005
diphenyl 1-[(N-benzoylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000058
diphenyl 1-[(N-naphthalenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.000006
diphenyl 1-[(N-o,o-dimethylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000044
diphenyl 1-[(N-o-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000066
diphenyl 1-[(N-p-bromobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000062
diphenyl 1-[(N-p-cyanobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000058
diphenyl 1-[(N-p-methoxybenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.000007
diphenyl 1-[(N-p-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000015
diphenyl 1-[(N2-thiophenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus;
-
pH 8.8, 37°C
0.0000031
diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
Homo sapiens;
-
pH 8.8, 37°C
0.0036
methyl 4'-(6-carbamoyl-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens;
-
pH 8.8, 37°C
0.0028
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxylate
Homo sapiens;
-
pH 8.8, 37°C
0.016
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-4-carboxylate
Homo sapiens;
-
pH 8.8, 37°C
0.016
methyl 4'-(naphthalene-2-sulfonamido)biphenyl-3-carboxylate
Homo sapiens;
-
pH 8.8, 37°C
0.0098
methyl 4'-(naphthalene-2-sulfonamido)biphenyl-4-carboxylate
Homo sapiens;
-
pH 8.8, 37°C
0.014
methyl 6-(3'-(methoxycarbonyl)biphenyl-4-ylcarbamoyl)-2-naphthoate
Homo sapiens;
-
pH 8.8, 37°C
0.008
N-(2,4'-dimethoxybiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
Homo sapiens;
-
pH 8.8, 37°C
0.008
N-(3',4'-dimethoxybiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
Homo sapiens;
-
pH 8.8, 37°C
0.062
N-(3'-aminobiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
Homo sapiens;
-
pH 8.8, 37°C
0.0012
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
Homo sapiens;
-
pH 8.8, 37°C
0.0064
N2-(2,4'-dimethoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens;
-
pH 8.8, 37°C
0.0024
N2-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens;
-
pH 8.8, 37°C
0.0029
N2-(3'-methoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens;
-
pH 8.8, 37°C
0.045
N2-(4-(aminomethyl)phenyl)naphthalene-2,6-dicarboxamide trifluoroacetate
Homo sapiens;
-
pH 8.8, 37°C
0.0081
[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]acetic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000098
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000098
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
Homo sapiens;
-
pH 8.8, 37°C
0.00024
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00024
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH 8.8, 37°C
0.000039
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000039
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens;
-
pH 8.8, 37°C
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
enzyme activity in different tissues with and without inhibitor treatment, overview
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
7.4
-
assay at
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
37
-
assay at
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
silencing of transmembrane protein Notch1 by siRNA results in significant reduction in the expression of uPA and matrix metalloproteinase-9 gene transcripts. Knock-down of Notch also reduces the mRNA expression and protein levels of uPA and matrix metalloproteinase-9
-
uPA shows extensive colocalization with alpha-granule proteins in both cultured Quebec platelet disease megakaryocytes and platelets, and with plasminogen in Quebec platelet disease platelets
-
standard model of the balloon catheter injury of the carotid. Periadventitial application of recombinant uPA significantly reduces lumen size and vessel area encompassed by the external lamina both 1 and 4 days after treatment.In fallatory cells accumulate in the arterial adventitia at both 1 and 4 days after uPA treatment. Four days after injury in uPA-treated arteries, 3 proinflammatory and 2 oxidation-related genes are differentially expressed
-
uPA, seprase and pipeptidylaminopeptidase IV immunoreactivity is found in dysplastic and cancer cells as well as in stromal cells adjacent to dysplasia and cancer sites, but not in normal epithelium. There is a significant association between uPA expression and sex, tumor size and histological classification in carcinomas. Squamous cell carcinoma lines display higher levels of uPA, seprase and dipeptidylaminopeptidase IV than normal esophageal epithelial cell lines
-
human recombinant uPA induces stem cell migration. Retrovirus-mediated overexpression of uPA and uPA receptor in neuroblastoma NB-1691 cells induced robust migration of stem cells toward NB-1691 cell-conditioned media, compared with media derived from wild-type NB-1691 cells. Depletion of uPA from PC-3 prostate cancer cell-conditioned medium blocks stem cell migration