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Information on EC 3.4.21.73 - u-Plasminogen activator
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3.4.21.73 u-Plasminogen activatorSpecify your search results
Word Map
- 3.4.21.73
-
fibrinolytic
- pai-1
- artery
-
thrombolysis
-
tissue-type
- metastasis
- fibrin
- endothelial
- clot
- inhibitor-1
- heparin
- infarct
- vein
- streptokinase
- myocardial
- venous
-
catheter
- thrombus
- fibrinogen
- embolism
- angiogenesis
- bleeding
- coronary
- hemorrhage
- coagulation
- metalloproteinases
-
anticoagulation
-
zymography
-
single-chain
- mmp-9
-
angioplasty
-
angiography
-
recanalization
-
patency
- thromboembolism
- vitronectin
-
percutaneous
-
thrombotic
- occlusions
-
transluminal
-
amidolytic
-
kringle
-
thrombectomy
-
pericellular
-
intraarterial
-
intracoronary
- alteplase
-
2-antiplasmin
-
reocclusion
-
euglobulin
- analysis
- diagnostics
- agriculture
- pharmacology
- drug development
- medicine
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Synonyms
urokinase, urokinase-type plasminogen activator, urokinase plasminogen activator, urokinase type plasminogen activator, urokinase-type pa, urokinase-type plasminogen, urokinase-plasminogen activator, urinary plasminogen activator, cellular plasminogen activator, two-chain urokinase-type plasminogen activator, 
more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
u-PA
uPA
Urokinase
Urokinase plasminogen activator
urokinase type plasminogen activator
urokinase-type PA
Urokinase-type plasminogen activator
uPA
-
-
669677, 683130, 683220, 683299, 683304, 683333, 683372, 683456, 683550, 683623, 683772, 707096, 707287, 707518, 707678, 707840, 707866, 707892, 707901, 707951, 707983, 708669, 708679, 708749, 708762, 708771, 709067, 709570, 709736, 709905, 709912, 710121, 710133, 710163, 710248, 710469, 710553, 710656, 717076, 717222, 717386, 717414, 717828, 717899, 718142, 718270, 718287, 731238, 731932, 732184
uPA
-
uPA
-
-
Urokinase plasminogen activator
-
-
Urokinase-type plasminogen activator
-
-
Urokinase-type plasminogen activator
-
Urokinase-type 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
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CAS REGISTRY NUMBER
COMMENTARY
139639-24-0
-
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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
-
?
D-Ile-Pro-Arg-4-nitroanilide + H2O
D-Ile-Pro-Arg + 4-nitroaniline
-
-
?
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-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
-
?
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 SUBSTRATE
NATURAL 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
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
-
-
?
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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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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INHIBITOR
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
-
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
-
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
-
human PAI-1
human plasminogen activator inhibitor-1, complex structure of uPA:PAI-1 Michaelis complex, interaction analysis, the S3-pocket-lining residues of uPA and the P3 residue of both PAI-1 and plasminogen form numerous polar interactions in the human uPA:PAI-1 Michaelis complex, overview
-
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-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
-
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
N2-(4-(aminomethyl)phenyl)naphthalene-2,6-dicarboxamide trifluoroacetate
-
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
-
-
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
-
-
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic 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-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]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic 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
-
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
-
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
although the interaction areas between protease-substrate and protease-inhibitor are shared, the two interactions are mechanistically different. Species specificity of the reaction of PAI-1 and uPA. Analysis of interaction kinetics of the wild-type and mutant human enzymes with human and zebrafish plasminogen activator inhibitor-1 and of the zebrafish wild-type and mutant enzyme with both inhibitors, overview
-
additional information
-
although the interaction areas between protease-substrate and protease-inhibitor are shared, the two interactions are mechanistically different. Species specificity of the reaction of PAI-1 and uPA. Analysis of interaction kinetics of the wild-type and mutant human enzymes with human and zebrafish plasminogen activator inhibitor-1 and of the zebrafish wild-type and mutant enzyme with both inhibitors, overview
-
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
-
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
-
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
-
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
0.438
L-diglutamyl-glycyl-L-arginine-4-nitroanilide
-
pH 8.8, nonphosphorylated uPA
0.608
L-diglutamyl-glycyl-L-arginine-4-nitroanilide
-
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-diglutamyl-glycyl-L-arginine-4-nitroanilide
-
pH 8.8, nonphosphorylated uPA
0.0113
L-diglutamyl-glycyl-L-arginine-4-nitroanilide
-
pH 7.5, nonphosphorylated uPA
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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
-
-
0.000139
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
pH 8.8, 37°C
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
0.013
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-prolinamide
-
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
0.0077
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
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
0.0026
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
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
0.031
methyl 4'-(6-amino-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
pH 8.8, 37°C
0.011
methyl 4'-(6-bromo-2-naphthamido)biphenyl-3-carboxylate
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
0.007
methyl 4'-(6-chloro-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
pH 8.8, 37°C
0.009
methyl 4'-(6-cyano-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
pH 8.8, 37°C
0.004
methyl 4'-(6-methoxy-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
0.031
N-(3',4'-dimethoxybiphenyl-4-yl)-6-methoxy-2-naphthamide
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
0.0081
N2-(3-chlorobiphenyl-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 8.8, 37°C
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
0.00024
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens
pH 8.8, 37°C
0.00024
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
0.000039
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
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
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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
7.5
8.8
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
37
-
assay at
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
brenda
-
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
-
-
brenda
commercial preparation of low-molecular weight uPA from American Diagnostica
-
-
brenda
high-molecular weight uPA expressed in SP2/0 cell culture from Abbott Biotech
-
-
brenda
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
-
-
brenda
recombinant amino-terminal fragment S1-E143 expressed in Pichia pastoris
-
-
brenda
recombinant plasmin-resistant mutant of single-chain uPA obtained by site-specific mutagenesis of Lys158 to Glu
-
-
brenda
recombinant single chain urokinase-type plasminogen activator is home-made by expression of uPA cDNA in Chinese hamster ovary cells
-
-
brenda
commercial preparation of low-molecular weight uPA from American Diagnostica
-
-
brenda
high-molecular weight uPA expressed in SP2/0 cell culture from Abbott Biotech
-
-
brenda
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
-
-
brenda
recombinant single chain urokinase-type plasminogen activator is home-made by expression of uPA cDNA in Chinese hamster ovary cells
-
-
brenda
-
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
-
-
brenda
mice model for kidney ischemia reperfusion injury and for acute kidney allograft rejection
-
-
brenda
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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
brenda
-
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
brenda
-
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
brenda
-
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
brenda
-
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
brenda
-
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
brenda
-
human lung cancer cell line H1415, activation of uPA and uPA receptor in malignant solid tumors augments neural and mesenchymal stem cell tropism. Expression levels of uPA receptor on human solid tumor cell linescorrelates with levels of uPA and soluble uPA receptor in tumor cell-conditioned media
brenda
-
subline of MDA-MB-231, stably transfected with the bacterial lacZ gene
brenda
-
CD34+ progenitor cells express normal amounts of uPA, while their differentiation into megakaryocytes results in abnormally increased expression of the uPA gene but not the flanking genes for vinculin or calcium/calmodulin-dependent protein kinase IIgamma on chromosome 10. 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
brenda
-
uPA localizes strongly to natural killer cells of the placental bed, especially at 8-10 weeks of gestation. uPA activity is similar in uterine natural killer cell culture supernatant compared with total unseparated decidual cells. uPA receptor in uterine natural killer cell lysates is significantly stronger than in total decidual cell lysates. Inhibitors PAI-1 and PAI-2 are not detected in uterine natural killer cell culture supernatants
brenda
-
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
brenda
-
activation of uPA and uPA receptor in malignant solid tumors augments neural and mesenchymal stem cell tropism. Expression levels of uPA receptor on human solid tumor cell lines correlates with levels of uPA and soluble uPA receptor in tumor cell-conditioned media
brenda
-
activation of uPA and uPA receptor in malignant solid tumors augments neural and mesenchymal stem cell tropism. Expression levels of uPA receptor on human solid tumor cell lines correlates with levels of uPA and soluble uPA receptor in tumor cell-conditioned media
brenda
-
study on cocaine-induced conditioned-place preference in rats with bilateral intra-accumbens injections of uPA-expressing lentiviral vectors. Overexpression of uPA in the nucleus accumbens significantly augments cocaine-induced place preference. Reinstatement with a low dose of cocaine produces significantly greater preference to the cocaine-associated context. Inhibition of tuPA expression using doxycycline abolishes the augmented acquisition produced by overexpression of uPA but not the expression of the cocaine-induced conditioned-place preference. Cocaine-induced cocaine-induced conditioned-place preference and reinstatement may be dependent on active extracellular uPA
brenda