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Information on EC 3.6.5.2 - small monomeric GTPase
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3.6.5.2 small monomeric GTPaseIUBMB Comments
A family of about 50 enzymes with a molecular mass of 21 kDa that are distantly related to the alpha-subunit of heterotrimeric G-protein GTPase (EC 3.6.5.1). They are involved in cell-growth regulation (Ras subfamily), membrane vesicle traffic and uncoating (Rab and ARF subfamilies), nuclear protein import (Ran subfamily) and organization of the cytoskeleton (Rho and Rac subfamilies).
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Word Map
- 3.6.5.2
- actin
- oncogene
- cytoskeleton
- pancreatic
- colorectal
- metastasis
- endosomes
- endothelial
- adenocarcinoma
- tumorigenesis
- carcinogenesis
-
gtp-bound
-
reorganization
- gdp
-
dominant-negative
- integrins
-
exocytosis
-
gtpase-activating
- synaptic
- phosphatidylinositol
- mapk
- erk
- vesicular
- microtubule
-
endocytic
- myosin
- filopodia
-
traffic
-
cell-cell
-
cytokinesis
-
neurite
- adenoma
- 3-kinase
-
protrusion
-
ruffle
-
rock
-
cargo
- lamellipodia
- proto-oncogene
-
prenylation
-
farnesylation
-
geranylgeranylation
-
farnesyltransferase
- aminoacyl-trnas
- actomyosin
- melanosomes
-
adherens
- raf
-
pleckstrin
- pharmacology
- medicine
- drug development
- cetuximab
- analysis
The enzyme appears in viruses and cellular organisms
Synonyms
k-ras, cdc42, h-ras, small gtpase, ef-tu, rho gtpase, rab11, rab3a, rab27a, rap1a, 
more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
ADP-ribosylation factor 6
Alp41
Alp41/Arl2
ARD1
-
ARF subfamily, stimulates cholera toxin ADP ribosyltransferase, involved in vesicular trafficking, key regulator for interaction of non-clathrin coat proteins with Golgi stacks and clathrin adaptor particles with the trans-Golgi network
Arf 1
Arf6
Cdc42
Der
Der GTPase
double Era-like protein
EF-Tu
FgCdc42
FgRac1
FgRHO1
FgRHO2
FgRHO3
FgRHO4
Gem
-
Ras-related, involved in receptor-mediated signal transduction at the plasma membrane
GTPase
GTPase Alp41/Arl2
Kir
-
Ras-related, involved in processes of invasion or metastasis in mammalia cells
monomeric G protein
monomeric GTPase
OsRac1
p21 ras
PRA
Pra2
Pra3
Rab1a
Rab1B
Rab2A
Rab2B
Rab6A
Rac
Rac-like GTP-binding protein 1
Rac1
Rac2
Rac3
Rad
RalA
Ran
RAP
Rap GTPase
Rap1
Rap1b
RAS
Ras GTPase
Ras proximity 1
Ras related GTPase Rap
Ras-associated protein 1
Rho
Rho family small GTPase
Rho GTPase
Rho1
RhoA
RhoB
rhoB p20
RhoGTPase
RhoH
ribosome-small-subunit-dependent GTPase A
RsgA
small GTPase
small GTPase Rac
small nuclear GTPase Ran
small Rho GTPase
vacuolar Rab GTPase
YjeQ
Ypt1
Ypt7p
additional information
Rho1
-
Rho1 is important for the localization of the Sec3 component of the exocyst complex
RhoH
initially named translation three four, RhoH is a GTPase-deficient so-called atypical Rho GTPase, RhoH is only found in vertebrates
RhoH
initially named translation three four, RhoH is a GTPase-deficient so-called atypical Rho GTPase, RhoH is only found in vertebrates
additional information
member of a novel small monomeric GTPase gene family
additional information
member of a novel small monomeric GTPase gene family
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
GTP + H2O = GDP + phosphate
A family of about 50 enzymes with a molecular mass of 21 kDa that are distantly related to the alpha-subunit of heterotrimeric G-protein GTPase, EC 3.6.1.46. They are involved in cell-growth regulation, Ras subfamily, membrane vesicle traffic and uncoating, Rab and ARF subfamilies, nuclear protein import, Ran subfamily, and organization of the cytoskeleton, Rho and Rac subfamilies
-
-
GTP + H2O = GDP + phosphate
a family of about 50 enzymes with a molecular mass of 21 kDa that are distantly related to the alpha-subunit of heterotrimeric G-protein GTPase, EC 3.6.1.46, they are involved in cell-growth regulation, Ras subfamily, membrane vesicle traffic and uncoating, Rab and ARF subfamilies, nuclear protein import, Ran subfamily, and organization of the cytoskeleton, Rho and Rac subfamilies
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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SYSTEMATIC NAME
IUBMB Comments
GTP phosphohydrolase (cell-regulating)
A family of about 50 enzymes with a molecular mass of 21 kDa that are distantly related to the alpha-subunit of heterotrimeric G-protein GTPase (EC 3.6.5.1). They are involved in cell-growth regulation (Ras subfamily), membrane vesicle traffic and uncoating (Rab and ARF subfamilies), nuclear protein import (Ran subfamily) and organization of the cytoskeleton (Rho and Rac subfamilies).
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CAS REGISTRY NUMBER
COMMENTARY
9059-32-9
-
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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
guanosine 5'-O-(3-thio)triphosphate + H2O
guanosine 5'-diphosphate + thiophosphate
-
-
-
?
p21-activated kinase 1 + H2O
activated p21-activated kinase 1 + ?
-
Gamide signals Rac/Cdc42 to activate p21-activated kinase 1
-
?
Rho-activated kinase + H2O
activated Rho-activated kinase + ?
-
Ggly signals Rac/Cdc42 to activate Rho-activated kinase
-
?
GTP + H2O
GDP + phosphate
-
the enzyme is involved in nucleocytoplasmic transport, mitotic spindle assembly and nuclear envelope formation. Nuclear import of Ran relies on a small RanGTP-binding protein, nuclear transport factor 2
-
?
GTP + H2O
GDP + phosphate
-
Arabidopsis thaliana circadian clock is regulated by the small GTPase LIP1. LIP1 plays a unique negative role in controlling circadian light input and is required for precise entrainment of the plant
-
?
GTP + H2O
GDP + phosphate
transport of precursor proteins across chloroplast membranes involves the GTPases Toc33/34 and Toc159 at the outer chloroplast envelope
-
?
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchange factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchanges factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
RHO-1 plays a role in hypodermal P cell migration to a ventral position during larval development
-
?
GTP + H2O
GDP + phosphate
GTP binds to Der in a cooperative manner and the interruption of cooperative nucleotide association disrupts the interaction of Der with the 50S subunit
-
?
GTP + H2O
GDP + phosphate
-
Rab11 plays a central role in the transport and secretion of pathogenic factors
-
?
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
GTP binds to Der in a cooperative manner and the interruption of cooperative nucleotide association disrupts the interaction of Der with the 50S subunit
-
?
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
Rac-1 coordinates changes in chondrocyte phenotype and function and stimulates the maturation process essential for skeletal development
-
?
GTP + H2O
GDP + phosphate
-
GhRac1 GTPase may be a potential regulator of fiber elongation by controlling cytoskeletal assembly
-
?
GTP + H2O
GDP + phosphate
-
-
-
?
GTP + H2O
GDP + phosphate
-
high affinity for GTP, significant GTPase activity
-
ir
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchange factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
cycling between the active GTP bound and the inactive GDP bound state, slow GTPase activity
-
ir
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchanges factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
Cdc42 causes formation of filopodia, which might be involved in the recognition of the extracellular environment
-
?
GTP + H2O
GDP + phosphate
Rab21 has a role in the dynamics of the early endocytic pathway
-
?
GTP + H2O
GDP + phosphate
-
Rab27a has a determinant role in melanocytes and lymphocytes, role in melanosome peripheral transfer, required for cytotoxic granule exocytosis
-
?
GTP + H2O
GDP + phosphate
-
Rac1 promotes actin polymerization and the formation of lamellipodia of migrating cells
-
?
GTP + H2O
GDP + phosphate
Rac1 regulates gene expression, cell cycle progression and rearrangement of the actin cytoskeleton, Rac1 is ubiquitously expressed and regulates a wide variety of cellular processes
-
?
GTP + H2O
GDP + phosphate
Rac2 may be responsible for the regulation of the oxidative burst in hematopoietic cells
-
?
GTP + H2O
GDP + phosphate
Rac3 is ubiquitously expressed and regulates a wide variety of cellular processes
-
?
GTP + H2O
GDP + phosphate
-
RhoA promotes actin-myosin contractility and, thereby, the formation of stress fibers and focal adhesions, regulating cell shape, attachment and motility
-
?
GTP + H2O
GDP + phosphate
-
intrinsic GTPase reaction mechanism, biphasic reaction
-
?
GTP + H2O
GDP + phosphate
nucleotide binding and hydrolysis properties, comparison with the properties of the Rac isoforms Rac1 and Rac2
-
?
GTP + H2O
GDP + phosphate
nucleotide binding and hydrolysis properties, comparison with the properties of the Rac isoforms Rac1 and Rac3, Rac2 structure, altered dynamics of Rac2 at the switch I region may be responsible for the differing biochemical properties compared with Rac1 and 3
-
?
GTP + H2O
GDP + phosphate
nucleotide binding and hydrolysis properties, comparison with the properties of the Rac isoforms Rac2 and Rac3, enzyme structure
-
?
GTP + H2O
GDP + phosphate
-
Trp-73 is a key position for interaction with the specific effectors of Rab27a, both in melanocytes and cytotoxic cells, Trp-73 is essential for the intrinsic GTPase activity, Gln-78 may stabilize the catalytic transition state between switch I and II
-
?
GTP + H2O
GDP + phosphate
RHEBL1 may play an important role in the NF-kappa B-mediated gene transcription
-
?
GTP + H2O
GDP + phosphate
-
tuberous sclerosis complex TSC2 displays activity of a GTPase-activating protein specifically towards the small G protein Rheb and inhibits its ability to stimulate the mTOR signalling pathway
-
?
GTP + H2O
GDP + phosphate
-
small GTPase Ral mediates SDF-1-induced migration of B cells and multiple myeloma cells
-
?
GTP + H2O
GDP + phosphate
-
small GTPases Rab5 and RalA regulate intracellular traffic of P-glycoprotein. Altering the intracellular trafficking of P-glycoprotein by modulation of its small GTPase regulators can be potential strategy to overcome multidrug resistance, a major obstacle in cancer chemotherapy
-
?
GTP + H2O
GDP + phosphate
-
small nuclear GTPase Ran controls the directionality of macromolecular transport between the nucleus and the cytoplasm. Ran has important roles during mitosis, when the nucleus is reorganized to allow chromosome segregation. Ran directs the assembly of the mitotic spindle, nuclear-envelope dynamics and the timing of cell-cycle transitions
-
?
GTP + H2O
GDP + phosphate
-
the small GTPase Rac plays a crucial role in activation of Nox2- and Nox1-based oxidases i all the possible combinations of the organizer p47phox or Noxo1 with the activator p67phox or Noxa1
-
?
GTP + H2O
GDP + phosphate
-
two conformational states of Ras GTPase exhibit differential GTP-binding kinetics
-
?
GTP + H2O
GDP + phosphate
enzyme Rheb contains a high basal GTP level
-
?
GTP + H2O
GDP + phosphate
-
-
-
?
GTP + H2O
GDP + phosphate
-
small nuclear GTPase Ran controls the directionality of macromolecular transport between the nucleus and the cytoplasm. Ran has important roles during mitosis, when the nucleus is reorganized to allow chromosome segregation. Ran directs the assembly of the mitotic spindle, nuclear-envelope dynamics and the timing of cell-cycle transitions
-
?
GTP + H2O
GDP + phosphate
-
two conformational states of Ras GTPase exhibit differential GTP-binding kinetics
-
?
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
acts on the intracellular membrane through the trafficking pathway
-
?
GTP + H2O
GDP + phosphate
transport of precursor proteins across chloroplast membranes involves the GTPases Toc33/34 and Toc159 at the outer chloroplast envelope
-
?
GTP + H2O
GDP + phosphate
-
small GTPase Rac-1 is a regulator of mesangial cell morphology and thrombospondin-1 expression
-
?
GTP + H2O
GDP + phosphate
-
Rnd1 is involved in signaling pathways of neuronal activity-dependent dendritic development
-
?
GTP + H2O
GDP + phosphate
-
Rho A-linked pathway important in the endothelin-1 signaling to c-fos SRC
-
ir
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchange factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchanges factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
Rho3p and Rho4p are involved in regulating cell polarity by controlling polarized exocytosis. It is proposed that Wsc1p participates in the regulation of a Rho3/4-dependent cellular mechanism
-
?
GTP + H2O
GDP + phosphate
-
GTP binds to Der in a cooperative manner and the interruption of cooperative nucleotide association disrupts the interaction of Der with the 50S subunit
-
?
GTP + H2O
GDP + phosphate
GTP binds to Der in a cooperative manner and the interruption of cooperative nucleotide association disrupts the interaction of Der with the 50S subunit
-
?
GTP + H2O
GDP + phosphate
nucleotide binding pocket and binding structures, overview
-
?
GTP + H2O
GDP + phosphate
-
GTPase TcRho1 is required for differentiation of epimastigote to trypomastigote forms during the parasite cell cycle. TcRho1 plays a conserved regulatory role in cell-substrate adhesion in both NIH-3T3 fibroblasts and Trypanosoma cruzi epimastigotes. TcRho1 may regulate the substrate-adhesion in Trypanosoma cruzi,a critical step for successful progression of the parasite life cycle
-
?
guanosine 5'-O-(3-thiotriphosphate) + H2O
guanosine 5'-O-diphosphate + thiophosphate
-
poorly hydrolyzable, GTP[S]-activated Rac1 and Cdc42, but not RhoA, stimulate activity of phospholipase C-beta2 protein in complex with Rho GDP dissociation inhibitor protein LyGDL
-
?
guanosine 5'-O-(3-thiotriphosphate) + H2O
guanosine 5'-O-diphosphate + thiophosphate
-
no detectable hydrolysis of GTP at the ARF domain p3, 35-40% of the GTP bound to ARD1 domain p8 hydrolyzed in 1 h at room temperature
-
?
guanosine 5'-O-(3-thiotriphosphate) + H2O
guanosine 5'-O-diphosphate + thiophosphate
-
poorly hydrolyzable, GTP[S]-activated Rac1 and Cdc42, but not RhoA, stimulate activity of phospholipase C-beta2 protein in complex with Rho GDP dissociation inhibitor protein LyGDL
-
?
guanosine 5'-O-(3-thiotriphosphate) + H2O
guanosine 5'-O-diphosphate + thiophosphate
-
-
-
?
additional information
?
-
-
role of small GTPases in endothelial cytoskeletal dynamics and the shear stress response
-
?
additional information
?
-
-
GTPase-mediated regulation of the unfolded protein response in Caenorhabditis elegans is dependent on the AAA+ ATPase CDC-48
-
?
additional information
?
-
-
small GTPase Rab2 functions in the removal of apoptotic cells
-
?
additional information
?
-
-
Campylobacter jejuni invade host target cells by a unique mechanism and the activation of the Rho GTPase members Rac1 and Cdc42 play a crucial role in this entry process
-
?
additional information
?
-
Rhb1 is involved in the cell wall integrity pathway via activation of mitogen-activated protein kinase Mkc1
-
?
additional information
?
-
-
Rhb1 is involved in the cell wall integrity pathway via activation of mitogen-activated protein kinase Mkc1
-
?
additional information
?
-
p21-activated kinase Cla4 is a major downstream partner of Rac. Rac has strong effect on hyphal morphology
-
?
additional information
?
-
-
p21-activated kinase Cla4 is a major downstream partner of Rac. Rac has strong effect on hyphal morphology
-
?
additional information
?
-
-
small GTPases are involved in chemotaxis
-
?
additional information
?
-
-
Rho1 activity is required for proper development of the circular visceral mesoderm upon which the gland migrates, Rho1 GTPase regulates salivary gland invagination by maintaining apical localization of Crumbs, Drosophila atypical protein kinase C and Stardust and that this occurs partially through regulation of Crumbs RNA level and apical localization of the transcript and by inducing apical constriction and cell shape change through Rho-kinase
-
?
additional information
?
-
-
crystal cell rupture after injury in Drosophila requires the JNK pathway, small GTPases and the TNF homolog Eiger
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
A0A098E0E9
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
A0A098E0E9
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
FgRac1 interacts with the PBD domain of FgCla4
-
?
additional information
?
-
RASL11A is down-regulated in prostate tumors and may have a tumor suppressor role in prostate cancer
-
?
additional information
?
-
RASL11A is down-regulated in prostate tumors and may have a tumor suppressor role in prostate cancer
-
?
additional information
?
-
-
RASL11A is down-regulated in prostate tumors and may have a tumor suppressor role in prostate cancer
-
?
additional information
?
-
-
Co-regulation of constitutive nitric oxide synthases and NADPH oxidase by the small GTPase Rac
-
?
additional information
?
-
-
small GTPase Rac is directly involved in activation of the superoxide-producing NADPH oxidase Nox1
-
?
additional information
?
-
-
the Ral-exocyst pathway participates in the regulation of platelet dense granule secretion by enhancing the Ca2+ sensitivity of the secretion
-
?
additional information
?
-
-
Rap1 plays a critical role in the regulation of beta1-integrin affinity, adhesion, and migration in endothelial cells and in postnatal neovascularization
-
?
additional information
?
-
-
Rho and Rac play a role in the regulation cytoskeletal remodeling and EC barrier regulation
-
?
additional information
?
-
-
RhoA activity is required for modulating cell migration and proliferation through cytoskeleton reorganization and focal adhesion formation in response to wounding
-
?
additional information
?
-
-
RhoA may serve as intermediary for functional receptor for thromboxane A2-signaling axis to regulate tumor cell motility
-
?
additional information
?
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
?
additional information
?
-
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
?
additional information
?
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
?
additional information
?
-
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
?
additional information
?
-
at least 3 mitogen-activated protein kinases (MAPKs) are direct targets of Rac1: MLK2, MLK3, and MEKK4
-
?
additional information
?
-
at least 3 mitogen-activated protein kinases (MAPKs) are direct targets of Rac1: MLK2, MLK3, and MEKK4
-
?
additional information
?
-
at least 3 mitogen-activated protein kinases (MAPKs) are direct targets of Rac1: MLK2, MLK3, and MEKK4
-
?
additional information
?
-
enzyme Rheb does not co-localize with microtubules but interacts with unpolymerized free alphabeta-tubulin, alphabeta-tubulin is a Rheb-binding protein. Rheb binds to deacetylated soluble alphabeta-tubulin
-
?
additional information
?
-
kinetic analysis of the GTPase nucleotide exchange reaction via homogeneous quenching resonance energy transfer assay, method development overview
-
?
additional information
?
-
kinetic analysis of the GTPase nucleotide exchange reaction via homogeneous quenching resonance energy transfer assay, method development overview
-
?
additional information
?
-
kinetic analysis of the GTPase nucleotide exchange reaction via homogeneous quenching resonance energy transfer assay, method development overview
-
?
additional information
?
-
binding of GppNHp by Rab8 leads to the active form of Rab8, like with GTP, but GppNHp is unhydrolyzable, binding studies
-
-
additional information
?
-
-
binding of GppNHp by Rab8 leads to the active form of Rab8, like with GTP, but GppNHp is unhydrolyzable, binding studies
-
-
additional information
?
-
-
Ras binds guanine nucleotides in its guanine nucleotide-binding cleft composed of G-box elements that are conserved among all GTPase proteins
-
-
additional information
?
-
-
Knock down of Rab21 impairs integrin-mediated cell adhesion and motility, its overexpression stimulates cell migration and cancer cell adhesion to collagen and human bone
-
?
additional information
?
-
-
in 3T3-L1 adipocytes, stimulation of lipolysis increases the association of Rab18 with lipid droplets, suggesting that recruitment of Rab18 is regulated by the metabolic state of individual lipid droplets
-
?
additional information
?
-
-
Rab and Ral GTPases function in exocyst assembly and vesicle-tethering processes, whereas the Rho family of GTPases functions in the local activation of the exocyst complex to facilitate downstream vesicle-fusion events
-
?
additional information
?
-
-
Rac GTPases play an important role in enucleation of mammalian erythroblasts
-
?
additional information
?
-
-
Rac1 and Cdc42 are not required for differentiation and migration of neural crest cells, but are essential for mitotic activity and cell-cycle control in neural crest cell target structures
-
?
additional information
?
-
-
Rac1 is a central regulator of rapid encoding of novel spatial information in vivo, Rac1 mutants display deficits in working/episodic-like memory in the delayed matching-to-place
-
?
additional information
?
-
-
Rac2 selectively controls phagosomal alkalinization and antigen crosspresentation in CD8+ dendritic cells, Rac2 determines the subcellular assembly of the NADPH oxidase complex to phagosomes in CD8+ cells whereas in CD8- cells Rac1 mediates the assembly of NOX2 at the plasma membrane
-
?
additional information
?
-
-
RalA is a critical component in biphasic insulin release from pancreatic beta cells
-
?
additional information
?
-
-
Rap1 plays a critical role in the regulation of beta1-integrin affinity, adhesion, and migration in endothelial cells and in postnatal neovascularization
-
?
additional information
?
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
?
additional information
?
-
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
?
additional information
?
-
-
the small GTPase RhoA is crucial for MC3T3-E1 osteoblastic cell survival
-
?
additional information
?
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
?
additional information
?
-
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
?
additional information
?
-
recombinant RhoA activity reduces Ba2+ currents through CaV2.1, CaV2.2 and CaV2.3 Ca2+ channels independently of CaVbeta subunit. This inhibition occurs independently of RGKs activity and without modification of biophysical properties and global level of expression of the channel subunit
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
?
additional information
?
-
interaction site of HsRac1 with p67phox, an essential component of the NADPH oxidase complex
-
?
additional information
?
-
-
interaction site of HsRac1 with p67phox, an essential component of the NADPH oxidase complex
-
?
additional information
?
-
no activity with unhydrolyzable GTPgammaS, which is used for association/dissociation and binding analysis
-
-
additional information
?
-
-
no activity with unhydrolyzable GTPgammaS, which is used for association/dissociation and binding analysis
-
-
additional information
?
-
-
Rac1 can interact with the PBD domain of p21-activated kinase 1 (PAK1)
-
-
additional information
?
-
-
RalA is a critical component in biphasic insulin release from pancreatic beta cells
-
?
additional information
?
-
-
Rho1p and its downstream regulatory pathways are involved in controlling cell size in Saccharomyces cerevisiae
-
?
additional information
?
-
Alp41 GTPase interacts with cofactor C, but with cofactor D, Alp1D, only when bound to GDP
-
?
additional information
?
-
-
Alp41 GTPase interacts with cofactor C, but with cofactor D, Alp1D, only when bound to GDP
-
?
additional information
?
-
Alp41 GTPase interacts with cofactor C, but with cofactor D, Alp1D, only when bound to GDP
-
?
additional information
?
-
-
RhoA activity is required for modulating cell migration and proliferation through cytoskeleton reorganization and focal adhesion formation in response to wounding
-
?
additional information
?
-
the enzyme interacts with tubulin and co-localises to the flagellar pocket with BBS1 when this protein is overexpressed
-
?
additional information
?
-
-
the enzyme interacts with tubulin and co-localises to the flagellar pocket with BBS1 when this protein is overexpressed
-
?
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
p21-activated kinase 1 + H2O
activated p21-activated kinase 1 + ?
-
Gamide signals Rac/Cdc42 to activate p21-activated kinase 1
-
-
?
Rho-activated kinase + H2O
activated Rho-activated kinase + ?
-
Ggly signals Rac/Cdc42 to activate Rho-activated kinase
-
-
?
GTP + H2O
GDP + phosphate
-
the enzyme is involved in nucleocytoplasmic transport, mitotic spindle assembly and nuclear envelope formation. Nuclear import of Ran relies on a small RanGTP-binding protein, nuclear transport factor 2
-
-
?
GTP + H2O
GDP + phosphate
-
Arabidopsis thaliana circadian clock is regulated by the small GTPase LIP1. LIP1 plays a unique negative role in controlling circadian light input and is required for precise entrainment of the plant
-
-
?
GTP + H2O
GDP + phosphate
transport of precursor proteins across chloroplast membranes involves the GTPases Toc33/34 and Toc159 at the outer chloroplast envelope
-
-
?
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchanges factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
RHO-1 plays a role in hypodermal P cell migration to a ventral position during larval development
-
-
?
GTP + H2O
GDP + phosphate
-
Rab11 plays a central role in the transport and secretion of pathogenic factors
-
-
?
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
Rac-1 coordinates changes in chondrocyte phenotype and function and stimulates the maturation process essential for skeletal development
-
-
?
GTP + H2O
GDP + phosphate
-
GhRac1 GTPase may be a potential regulator of fiber elongation by controlling cytoskeletal assembly
-
-
?
GTP + H2O
GDP + phosphate
-
high affinity for GTP, significant GTPase activity
-
ir
GTP + H2O
GDP + phosphate
-
cycling between the active GTP bound and the inactive GDP bound state, slow GTPase activity
-
ir
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchanges factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
Cdc42 causes formation of filopodia, which might be involved in the recognition of the extracellular environment
-
-
?
GTP + H2O
GDP + phosphate
Rab21 has a role in the dynamics of the early endocytic pathway
-
-
?
GTP + H2O
GDP + phosphate
-
Rab27a has a determinant role in melanocytes and lymphocytes, role in melanosome peripheral transfer, required for cytotoxic granule exocytosis
-
-
?
GTP + H2O
GDP + phosphate
-
Rac1 promotes actin polymerization and the formation of lamellipodia of migrating cells
-
-
?
GTP + H2O
GDP + phosphate
Rac1 regulates gene expression, cell cycle progression and rearrangement of the actin cytoskeleton, Rac1 is ubiquitously expressed and regulates a wide variety of cellular processes
-
-
?
GTP + H2O
GDP + phosphate
Rac2 may be responsible for the regulation of the oxidative burst in hematopoietic cells
-
-
?
GTP + H2O
GDP + phosphate
Rac3 is ubiquitously expressed and regulates a wide variety of cellular processes
-
-
?
GTP + H2O
GDP + phosphate
-
RhoA promotes actin-myosin contractility and, thereby, the formation of stress fibers and focal adhesions, regulating cell shape, attachment and motility
-
-
?
GTP + H2O
GDP + phosphate
RHEBL1 may play an important role in the NF-kappa B-mediated gene transcription
-
-
?
GTP + H2O
GDP + phosphate
-
tuberous sclerosis complex TSC2 displays activity of a GTPase-activating protein specifically towards the small G protein Rheb and inhibits its ability to stimulate the mTOR signalling pathway
-
-
?
GTP + H2O
GDP + phosphate
-
small GTPase Ral mediates SDF-1-induced migration of B cells and multiple myeloma cells
-
-
?
GTP + H2O
GDP + phosphate
-
small GTPases Rab5 and RalA regulate intracellular traffic of P-glycoprotein. Altering the intracellular trafficking of P-glycoprotein by modulation of its small GTPase regulators can be potential strategy to overcome multidrug resistance, a major obstacle in cancer chemotherapy
-
-
?
GTP + H2O
GDP + phosphate
-
small nuclear GTPase Ran controls the directionality of macromolecular transport between the nucleus and the cytoplasm. Ran has important roles during mitosis, when the nucleus is reorganized to allow chromosome segregation. Ran directs the assembly of the mitotic spindle, nuclear-envelope dynamics and the timing of cell-cycle transitions
-
-
?
GTP + H2O
GDP + phosphate
-
the small GTPase Rac plays a crucial role in activation of Nox2- and Nox1-based oxidases i all the possible combinations of the organizer p47phox or Noxo1 with the activator p67phox or Noxa1
-
-
?
GTP + H2O
GDP + phosphate
enzyme Rheb contains a high basal GTP level
-
-
?
GTP + H2O
GDP + phosphate
-
small nuclear GTPase Ran controls the directionality of macromolecular transport between the nucleus and the cytoplasm. Ran has important roles during mitosis, when the nucleus is reorganized to allow chromosome segregation. Ran directs the assembly of the mitotic spindle, nuclear-envelope dynamics and the timing of cell-cycle transitions
-
-
?
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
acts on the intracellular membrane through the trafficking pathway
-
-
?
GTP + H2O
GDP + phosphate
transport of precursor proteins across chloroplast membranes involves the GTPases Toc33/34 and Toc159 at the outer chloroplast envelope
-
-
?
GTP + H2O
GDP + phosphate
-
small GTPase Rac-1 is a regulator of mesangial cell morphology and thrombospondin-1 expression
-
-
?
GTP + H2O
GDP + phosphate
-
Rho A-linked pathway important in the endothelin-1 signaling to c-fos SRC
-
ir
GTP + H2O
GDP + phosphate
-
increased rate of nucleotide dissociation by interaction with guanosine exchanges factors that facilitates loading with GTP
-
ir
GTP + H2O
GDP + phosphate
-
unidirectional cycle in which exchange of GDP for GTP turns on a switch and GTP hydrolysis turns it off
-
ir
GTP + H2O
GDP + phosphate
-
Rho3p and Rho4p are involved in regulating cell polarity by controlling polarized exocytosis. It is proposed that Wsc1p participates in the regulation of a Rho3/4-dependent cellular mechanism
-
-
?
additional information
?
-
-
role of small GTPases in endothelial cytoskeletal dynamics and the shear stress response
-
-
?
additional information
?
-
-
GTPase-mediated regulation of the unfolded protein response in Caenorhabditis elegans is dependent on the AAA+ ATPase CDC-48
-
-
?
additional information
?
-
-
small GTPase Rab2 functions in the removal of apoptotic cells
-
-
?
additional information
?
-
-
Campylobacter jejuni invade host target cells by a unique mechanism and the activation of the Rho GTPase members Rac1 and Cdc42 play a crucial role in this entry process
-
-
?
additional information
?
-
Rhb1 is involved in the cell wall integrity pathway via activation of mitogen-activated protein kinase Mkc1
-
-
?
additional information
?
-
-
Rhb1 is involved in the cell wall integrity pathway via activation of mitogen-activated protein kinase Mkc1
-
-
?
additional information
?
-
p21-activated kinase Cla4 is a major downstream partner of Rac. Rac has strong effect on hyphal morphology
-
-
?
additional information
?
-
-
p21-activated kinase Cla4 is a major downstream partner of Rac. Rac has strong effect on hyphal morphology
-
-
?
additional information
?
-
-
small GTPases are involved in chemotaxis
-
-
?
additional information
?
-
-
Rho1 activity is required for proper development of the circular visceral mesoderm upon which the gland migrates, Rho1 GTPase regulates salivary gland invagination by maintaining apical localization of Crumbs, Drosophila atypical protein kinase C and Stardust and that this occurs partially through regulation of Crumbs RNA level and apical localization of the transcript and by inducing apical constriction and cell shape change through Rho-kinase
-
-
?
additional information
?
-
-
crystal cell rupture after injury in Drosophila requires the JNK pathway, small GTPases and the TNF homolog Eiger
-
-
?
additional information
?
-
RASL11A is down-regulated in prostate tumors and may have a tumor suppressor role in prostate cancer
-
-
?
additional information
?
-
RASL11A is down-regulated in prostate tumors and may have a tumor suppressor role in prostate cancer
-
-
?
additional information
?
-
-
RASL11A is down-regulated in prostate tumors and may have a tumor suppressor role in prostate cancer
-
-
?
additional information
?
-
-
Co-regulation of constitutive nitric oxide synthases and NADPH oxidase by the small GTPase Rac
-
-
?
additional information
?
-
-
small GTPase Rac is directly involved in activation of the superoxide-producing NADPH oxidase Nox1
-
-
?
additional information
?
-
-
the Ral-exocyst pathway participates in the regulation of platelet dense granule secretion by enhancing the Ca2+ sensitivity of the secretion
-
-
?
additional information
?
-
-
Rap1 plays a critical role in the regulation of beta1-integrin affinity, adhesion, and migration in endothelial cells and in postnatal neovascularization
-
-
?
additional information
?
-
-
Rho and Rac play a role in the regulation cytoskeletal remodeling and EC barrier regulation
-
-
?
additional information
?
-
-
RhoA activity is required for modulating cell migration and proliferation through cytoskeleton reorganization and focal adhesion formation in response to wounding
-
-
?
additional information
?
-
-
RhoA may serve as intermediary for functional receptor for thromboxane A2-signaling axis to regulate tumor cell motility
-
-
?
additional information
?
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
-
?
additional information
?
-
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
-
?
additional information
?
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
-
?
additional information
?
-
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
-
?
additional information
?
-
at least 3 mitogen-activated protein kinases (MAPKs) are direct targets of Rac1: MLK2, MLK3, and MEKK4
-
-
?
additional information
?
-
at least 3 mitogen-activated protein kinases (MAPKs) are direct targets of Rac1: MLK2, MLK3, and MEKK4
-
-
?
additional information
?
-
at least 3 mitogen-activated protein kinases (MAPKs) are direct targets of Rac1: MLK2, MLK3, and MEKK4
-
-
?
additional information
?
-
enzyme Rheb does not co-localize with microtubules but interacts with unpolymerized free alphabeta-tubulin, alphabeta-tubulin is a Rheb-binding protein. Rheb binds to deacetylated soluble alphabeta-tubulin
-
-
?
additional information
?
-
-
Knock down of Rab21 impairs integrin-mediated cell adhesion and motility, its overexpression stimulates cell migration and cancer cell adhesion to collagen and human bone
-
-
?
additional information
?
-
-
in 3T3-L1 adipocytes, stimulation of lipolysis increases the association of Rab18 with lipid droplets, suggesting that recruitment of Rab18 is regulated by the metabolic state of individual lipid droplets
-
-
?
additional information
?
-
-
Rab and Ral GTPases function in exocyst assembly and vesicle-tethering processes, whereas the Rho family of GTPases functions in the local activation of the exocyst complex to facilitate downstream vesicle-fusion events
-
-
?
additional information
?
-
-
Rac GTPases play an important role in enucleation of mammalian erythroblasts
-
-
?
additional information
?
-
-
Rac1 and Cdc42 are not required for differentiation and migration of neural crest cells, but are essential for mitotic activity and cell-cycle control in neural crest cell target structures
-
-
?
additional information
?
-
-
Rac1 is a central regulator of rapid encoding of novel spatial information in vivo, Rac1 mutants display deficits in working/episodic-like memory in the delayed matching-to-place
-
-
?
additional information
?
-
-
Rac2 selectively controls phagosomal alkalinization and antigen crosspresentation in CD8+ dendritic cells, Rac2 determines the subcellular assembly of the NADPH oxidase complex to phagosomes in CD8+ cells whereas in CD8- cells Rac1 mediates the assembly of NOX2 at the plasma membrane
-
-
?
additional information
?
-
-
RalA is a critical component in biphasic insulin release from pancreatic beta cells
-
-
?
additional information
?
-
-
Rap1 plays a critical role in the regulation of beta1-integrin affinity, adhesion, and migration in endothelial cells and in postnatal neovascularization
-
-
?
additional information
?
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
-
?
additional information
?
-
-
RhoH inhibits IkappaB degradation and acts as a specific negative regulator for Rac and RhoA-induced p38 activity
-
-
?
additional information
?
-
-
the small GTPase RhoA is crucial for MC3T3-E1 osteoblastic cell survival
-
-
?
additional information
?
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
-
?
additional information
?
-
-
the small GTPase RhoH is an atypical regulator of haematopoietic cells
-
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
-
?
additional information
?
-
Ras-related, small GTPases act as molecular switches that control a variety of cellular processes by cycling between alternative conformational states: in the active state, they are bound with GTP, and in the inactive state, they are bound with GDP. In their active state, GTPases recognize their target effector proteins and evoke responses until GTP hydrolysis returns the switch to the off position
-
-
?
additional information
?
-
interaction site of HsRac1 with p67phox, an essential component of the NADPH oxidase complex
-
-
?
additional information
?
-
-
interaction site of HsRac1 with p67phox, an essential component of the NADPH oxidase complex
-
-
?
additional information
?
-
-
Rac1 can interact with the PBD domain of p21-activated kinase 1 (PAK1)
-
-
-
additional information
?
-
-
RalA is a critical component in biphasic insulin release from pancreatic beta cells
-
-
?
additional information
?
-
-
Rho1p and its downstream regulatory pathways are involved in controlling cell size in Saccharomyces cerevisiae
-
-
?
additional information
?
-
Alp41 GTPase interacts with cofactor C, but with cofactor D, Alp1D, only when bound to GDP
-
-
?
additional information
?
-
-
Alp41 GTPase interacts with cofactor C, but with cofactor D, Alp1D, only when bound to GDP
-
-
?
additional information
?
-
Alp41 GTPase interacts with cofactor C, but with cofactor D, Alp1D, only when bound to GDP
-
-
?
additional information
?
-
-
RhoA activity is required for modulating cell migration and proliferation through cytoskeleton reorganization and focal adhesion formation in response to wounding
-
-
?
additional information
?
-
the enzyme interacts with tubulin and co-localises to the flagellar pocket with BBS1 when this protein is overexpressed
-
-
?
additional information
?
-
-
the enzyme interacts with tubulin and co-localises to the flagellar pocket with BBS1 when this protein is overexpressed
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
Mg2+
Mg2+
-
coordinated to oxygens of beta- and gamma-phosphates of GTP, essential for GTP hydrolysis
Mg2+
-
in absence of Mg2+ rapid release of GDP but dissociation rate of GTP very slow
Mg2+
-
the Mg2+ cofactor acts as a stabilizer for the bound nucleotides by slowing down the off and on rates, Mg2+ has only a minor effect on the intrinsic hydrolysis rate of GTP, kinetic study of the interaction of GTP with Cdc42 in the absence and presence of Mg2+
Mg2+
nucleotide binding to Ras is greatly enhanced by Mg2+
Mg2+
-
1 mM required for optimal activity, involved in binding of beta- and gamma-phosphates of GTP
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2E)-2-[(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
inhibition of GEF-Rac1 interaction (selective for Trio)
2-(morpholin-4-ylmethyl)-5-[(5-[[7-(trifluoromethyl)quinolin-4-yl]sulfanyl]pentyl)oxy]-4H-pyran-4-one
inhibition of Rac1 nucleotide binding possiblly using an allosteric mechanism
2-amino-8-hydroxy-9-[3-hydroxy-2-(hydroxymethyl)cyclopentyl]-5,9-dihydro-6H-purin-6-one
inhibition of Rac1-dependent NADPH oxidase activity
3-(2-hydroxyphenyl)-N-[4-(piperidin-1-ylsulfonyl)phenyl]-1H-pyrazole-5-carboxamide
inhibition of GEF-Rac1 interaction (Tiam1, Trio, and Vav2), the compound inhibits lamellipodia formation and smooth muscle cell migration
3-([(2E)-2-cyano-3-(4-methoxy-3-[(naphthalen-1-ylcarbonyl)oxy]phenyl)prop-2-enoyl]amino)benzoic acid
5-(3-chloro-4-[(3-fluorobenzyl)oxy]-5-methoxybenzyl)-1-(4-hydroxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione
5-chloro-3-(2-oxo-2-(4-[3-(trifluoromethyl)phenyl]piperazin-1-yl)ethyl)-1H-indole-2-carboxylic acid
9-methoxy-5-(3-nitrophenyl)-2-phenyl-3,10b-dihydropyrazolo[1,5-c][1,3]benzoxazine
inhibition of effector-Rac1 interaction (p67phox)
atorvastatin
-
marketed as Lipitor, i.e. [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, inhibits RhoA activity by reducing Rho geranylgeranylation
Calmodulin
-
binding of calmodulin to GST-immobilized Kir/Gem peptide inhibits GTP binding
cerivastatin
-
marketed as Baycol/Lipobay, i.e. (E,3R,5S)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-dipropan-2-yl-pyridin-3-yl]-3,5-dihydroxy-hept-6-enoic acid, RhoA inhibitor
EDTA
inhibits nucleotide binding to Ras; inhibits nucleotide binding to Ras; inhibits nucleotide binding to Ras
ethyl ([2-(2-methoxy-4-((Z)-[1-(4-methylphenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl)phenoxy)ethyl]sulfanyl)acetate
GTPgammaS
-
Arl6 is competitively inhibited by the increasing concentrations of non-radioactive GTPgammaS
lovastatin
-
marketed as Mevacor, i.e. 8-[2-(4-hydroxy-6-oxo-oxan-2-yl)ethyl]-3,7-dimethyl-1,2,3,7,8,8a-[hexahydronaphthalen-1-yl]2-methylbutanoate
N-(2-chlorobenzyl)-N-[[(4-methylphenyl)sulfonyl]carbamoyl]-L-alanine
-
Rho toxin from Clostridium botulinum, ADP-ribosylates and specifically inactivates rho-1
N-[4-methoxy-3-(piperidin-1-ylsulfonyl)phenyl]-1H-indazole-3-carboxamide
inhibition of GEF-Rac1 interaction (Tiam1)
N4-(9-ethyl-9H-carbazol-3-yl)-N2-[3-(morpholin-4-yl)propyl]pyrimidine-2,4-diamine
inhibition of GEF-Rac1 interaction (selective for Vav2)
N6-(2-[[5-(diethylamino)pentan-2-yl]amino]-6-methylpyrimidin-4-yl)-2-methylquinoline-4,6-diamine
a selective inhibitor for Rac1. The small molecule fits into the surface groove of Rac1 involved in the binding with GEFs, thus interfering with the Tiam1-Rac1 interaction
p21 activated kinase
PAK, inhibits nucleotide dissociation from enzyme; PAK, inhibits nucleotide dissociation from enzyme
-
PlexA
plexins (Plexs) comprise a large family of cell surface receptors for semaphorins (Semas) that function as evolutionarily conserved guidance molecules. Rap GTPase but not Ras GTPase homologs are inactivated by the GAP activity of several vertebrate plexins. GTPase activating protein (GAP) activity for Ras family small GTPases has been implicated in plexin signaling cascades through its RasGAP domain. Neuronal expression of mutant PlexA robustly restores defasciculation defects in PlexA null mutants when the catalytic arginine fingers of the PlexA RasGAP domain critical for GAP activity are disrupted. Deleting the RasGAP domain abolishes the ability of PlexA to rescue the PlexA guidance phenotypes. PlexA-mediated motor axon guidance is dependent on the presence of the PlexA RasGAP domain, but not on its GAP activity toward Ras family small GTPases
-
Rap1Gap
-
the GTPase activating protein catalyzes the hydrolysis of GTP by its asparagine side chain rendering Rap1 inactive
-
simvastatin
-
marketed as Zocor, i.e. [(1S,3R,7R,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxo-oxan-2-yl]ethyl]3.7-dimethyl]-1,2,3,7,8,8a-[hexahydronaphthalen-1-yl]2,2-dimethylbutanoate
statin
improves redox state in saphenous vein grafts in patients undergoing to coronary artery bypass grafting by inhibiting Rac1-mediated activation of NADPH oxidase
Yersinia outer protein T
-
Yersinia outer protein T is a cysteine protease that cleaves Rho protein directly upstream of the post-translationally modified cysteine, thereby releasing the GTPase from the membrane leading to inactivation, farnesylated RhoA is a preferred substrate of Yersinia outer protein T compared with the geranylgeranylated GTPase, geranylgeranylated RhoA, however, is the preferred substrate for Yersinia outer protein T-catalyzed cleavage with a 3fold faster turnover rate over Rac and Cdc42
-
3-([(2E)-2-cyano-3-(4-methoxy-3-[(naphthalen-1-ylcarbonyl)oxy]phenyl)prop-2-enoyl]amino)benzoic acid
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
3-([(2E)-2-cyano-3-(4-methoxy-3-[(naphthalen-1-ylcarbonyl)oxy]phenyl)prop-2-enoyl]amino)benzoic acid
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
3-([(2E)-2-cyano-3-(4-methoxy-3-[(naphthalen-1-ylcarbonyl)oxy]phenyl)prop-2-enoyl]amino)benzoic acid
-
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
3-([(2E)-2-cyano-3-(4-methoxy-3-[(naphthalen-1-ylcarbonyl)oxy]phenyl)prop-2-enoyl]amino)benzoic acid
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
5-(3-chloro-4-[(3-fluorobenzyl)oxy]-5-methoxybenzyl)-1-(4-hydroxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
5-(3-chloro-4-[(3-fluorobenzyl)oxy]-5-methoxybenzyl)-1-(4-hydroxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
5-(3-chloro-4-[(3-fluorobenzyl)oxy]-5-methoxybenzyl)-1-(4-hydroxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-(3-chloro-4-[(3-fluorobenzyl)oxy]-5-methoxybenzyl)-1-(4-hydroxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
5-chloro-3-(2-oxo-2-(4-[3-(trifluoromethyl)phenyl]piperazin-1-yl)ethyl)-1H-indole-2-carboxylic acid
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
5-chloro-3-(2-oxo-2-(4-[3-(trifluoromethyl)phenyl]piperazin-1-yl)ethyl)-1H-indole-2-carboxylic acid
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
5-chloro-3-(2-oxo-2-(4-[3-(trifluoromethyl)phenyl]piperazin-1-yl)ethyl)-1H-indole-2-carboxylic acid
-
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
5-chloro-3-(2-oxo-2-(4-[3-(trifluoromethyl)phenyl]piperazin-1-yl)ethyl)-1H-indole-2-carboxylic acid
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
ethyl ([2-(2-methoxy-4-((Z)-[1-(4-methylphenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl)phenoxy)ethyl]sulfanyl)acetate
-
ethyl ([2-(2-methoxy-4-((Z)-[1-(4-methylphenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl)phenoxy)ethyl]sulfanyl)acetate
-
ethyl ([2-(2-methoxy-4-((Z)-[1-(4-methylphenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl)phenoxy)ethyl]sulfanyl)acetate
-
-
ethyl ([2-(2-methoxy-4-((Z)-[1-(4-methylphenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl)phenoxy)ethyl]sulfanyl)acetate
-
GDP
the activation state of Rac1 depends on the release of guanosine diphosphate and the binding of guanosine triphosphate. This cycling is regulated by the guanine nucleotide exchange factors, as activators, and by the GTPase activating proteins; the activation state of Rac1 depends on the release of guanosine diphosphate and the binding of guanosine triphosphate. This cycling is regulated by the guanine nucleotide exchange factors, as activators, and by the GTPase activating proteins; the activation state of Rac1 depends on the release of guanosine diphosphate and the binding of guanosine triphosphate. This cycling is regulated by the guanine nucleotide exchange factors, as activators, and by the GTPase activating proteins
GDP
Rab proteins exist in the active GTP-bound and inactive GDP-bound conformations with the GTP/GDP exchange mediated by GTP exchange factors (GEF53) and it is the GTP-bound active form of Rab that promotes membrane trafficking upon interaction with effector proteins
guanine nucleotide dissociation inhibitor GDI
-
inhibits the dissociation of GDP from and the binding of GTP to rhoB p20
-
guanine nucleotide dissociation inhibitor GDI
-
down-regulating GTPase activity, inhibition of nucleotide dissociation
-
guanine nucleotide dissociation inhibitor GDI
-
down-regulating GTPase activity, inhibition of nucleotide dissociation
-
guanine nucleotide dissociation inhibitor GDI
-
down-regulating GTPase activity, inhibition of nucleotide dissociation
-
N-(2-acetylphenyl)-4-([2-(4-chloro-2-methylphenoxy)propanoyl]amino)benzamide
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
N-(2-acetylphenyl)-4-([2-(4-chloro-2-methylphenoxy)propanoyl]amino)benzamide
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
N-(2-acetylphenyl)-4-([2-(4-chloro-2-methylphenoxy)propanoyl]amino)benzamide
-
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
N-(2-acetylphenyl)-4-([2-(4-chloro-2-methylphenoxy)propanoyl]amino)benzamide
the compound is both biologically active against bacterial cells and a putative enzymatic inhibitor of Der GTPase homologue
additional information
-
exposure of confluent lung endothelial cell monolayers to wild type Pseudomonase aeruginosa strain PAK causes a significant decrease in Rac1 activity within 10 min
-
additional information
structure-based design of enzyme Der inhibitors using the X-ray crystal structure of Thermotoga maritima Der, computer-aided pharmacophore modeling. Analysis of the interactions of the inhibitory compounds with the Der GTP-binding site to understand the mechanism of inhibition. No or poor inhibition by 3-[(4Z)-5-hydroxy-3-methyl-4-([5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene)-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 3-[(4Z)-4-([5-(3-acetylphenyl)furan-2-yl]methylidene)-5-hydroxy-3-methyl-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 2-((Z)-[3-(4-carboxyphenyl)-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene]methyl)benzoic acid, (4E)-4-(2-[2-(3-methoxyphenoxy)ethoxy]benzylidene)-1-phenylpyrazolidine-3,5-dione, 3,4-bis([(3,4-dimethylphenoxy)acetyl]amino)benzoic acid, 2-(5,5-dimethyl-3-methylidenehexyl)-1-methyl-5-(3-adamantylbutyl)-3-propylbenzene, and 2-(3-([((2-[2-(dimethylamino)ethyl]-1H-indol-3-yl)methyl)sulfanyl]methyl)-5-methyl-1H-indol-2-yl)-N,N-dimethylethanamine
-
additional information
structure-based design of enzyme Der inhibitors using the X-ray crystal structure of Thermotoga maritima Der, computer-aided pharmacophore modeling. Analysis of the interactions of the inhibitory compounds with the Der GTP-binding site to understand the mechanism of inhibition. No or poor inhibition by 3-[(4Z)-5-hydroxy-3-methyl-4-([5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene)-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 3-[(4Z)-4-([5-(3-acetylphenyl)furan-2-yl]methylidene)-5-hydroxy-3-methyl-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 2-((Z)-[3-(4-carboxyphenyl)-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene]methyl)benzoic acid, (4E)-4-(2-[2-(3-methoxyphenoxy)ethoxy]benzylidene)-1-phenylpyrazolidine-3,5-dione, 3,4-bis([(3,4-dimethylphenoxy)acetyl]amino)benzoic acid, 2-(5,5-dimethyl-3-methylidenehexyl)-1-methyl-5-(3-adamantylbutyl)-3-propylbenzene, and 2-(3-([((2-[2-(dimethylamino)ethyl]-1H-indol-3-yl)methyl)sulfanyl]methyl)-5-methyl-1H-indol-2-yl)-N,N-dimethylethanamine
-
additional information
-
regulation of Cdc42 activity; regulation of Rac1 activity; regulation of RhoA activity
-
additional information
accumulation of acetylated alpha-tubulin by TSA treatment decreases the phosphorylation level of S6K1
-
additional information
three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity; three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity; three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity
-
additional information
three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity; three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity; three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity
-
additional information
three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity; three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity; three categories of selective Rac1 inhibitors affect different steps of the GTP/GDP pathway of enzyme activation: antagonists of Rac1-guanine nucleotide exchange factor interaction, allosteric inhibitors of nucleotide binding to Rac1, and antagonists of Rac1-mediated NADPH oxidase activity
-
additional information
Rab proteins are members of the Ras superfamily of GTPases that switch between GDP-bound (inactive) and GTP-bound (active) forms
-
additional information
-
Rab proteins are members of the Ras superfamily of GTPases that switch between GDP-bound (inactive) and GTP-bound (active) forms
-
additional information
most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation; most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation; most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation
-
additional information
most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation; most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation; most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation
-
additional information
most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation; most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation; most RhoGTPases bind to chaperones, called guanine nucleotide dissociation inhibitors (RhoGDIs), which are cytosolic proteins that lack enzymatic activity. GDIs retain RhoGTPases in the inactive conformation, sequester them from cellular membranes and protect the GTPase from effector binding and proteolytic degradation
-
additional information
-
RhoE downregulates the activity of RhoA by activating p190RhoGAP
-
additional information
RhoA- or ROCK-induced inhibitions are partially relieved upon incubation of the oocytes with the ROCK inhibitor Y27632
-
additional information
-
structure-based design of enzyme Der inhibitors using the X-ray crystal structure of Thermotoga maritima Der, computer-aided pharmacophore modeling. Analysis of the interactions of the inhibitory compounds with the Der GTP-binding site to understand the mechanism of inhibition. No or poor inhibition by 3-[(4Z)-5-hydroxy-3-methyl-4-([5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene)-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 3-[(4Z)-4-([5-(3-acetylphenyl)furan-2-yl]methylidene)-5-hydroxy-3-methyl-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 2-((Z)-[3-(4-carboxyphenyl)-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene]methyl)benzoic acid, (4E)-4-(2-[2-(3-methoxyphenoxy)ethoxy]benzylidene)-1-phenylpyrazolidine-3,5-dione, 3,4-bis([(3,4-dimethylphenoxy)acetyl]amino)benzoic acid, 2-(5,5-dimethyl-3-methylidenehexyl)-1-methyl-5-(3-adamantylbutyl)-3-propylbenzene, and 2-(3-([((2-[2-(dimethylamino)ethyl]-1H-indol-3-yl)methyl)sulfanyl]methyl)-5-methyl-1H-indol-2-yl)-N,N-dimethylethanamine
-
additional information
structure-based design of enzyme Der inhibitors using the X-ray crystal structure of Thermotoga maritima Der, computer-aided pharmacophore modeling. Analysis of the interactions of the inhibitory compounds with the Der GTP-binding site to understand the mechanism of inhibition. No or poor inhibition by 3-[(4Z)-5-hydroxy-3-methyl-4-([5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene)-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 3-[(4Z)-4-([5-(3-acetylphenyl)furan-2-yl]methylidene)-5-hydroxy-3-methyl-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 2-((Z)-[3-(4-carboxyphenyl)-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene]methyl)benzoic acid, (4E)-4-(2-[2-(3-methoxyphenoxy)ethoxy]benzylidene)-1-phenylpyrazolidine-3,5-dione, 3,4-bis([(3,4-dimethylphenoxy)acetyl]amino)benzoic acid, 2-(5,5-dimethyl-3-methylidenehexyl)-1-methyl-5-(3-adamantylbutyl)-3-propylbenzene, and 2-(3-([((2-[2-(dimethylamino)ethyl]-1H-indol-3-yl)methyl)sulfanyl]methyl)-5-methyl-1H-indol-2-yl)-N,N-dimethylethanamine
-
additional information
-
structure-based design of enzyme Der inhibitors using the X-ray crystal structure of Thermotoga maritima Der, computer-aided pharmacophore modeling. Analysis of the interactions of the inhibitory compounds with the Der GTP-binding site to understand the mechanism of inhibition. No or poor inhibition by 3-[(4Z)-5-hydroxy-3-methyl-4-([5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene)-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 3-[(4Z)-4-([5-(3-acetylphenyl)furan-2-yl]methylidene)-5-hydroxy-3-methyl-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid, 2-((Z)-[3-(4-carboxyphenyl)-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene]methyl)benzoic acid, (4E)-4-(2-[2-(3-methoxyphenoxy)ethoxy]benzylidene)-1-phenylpyrazolidine-3,5-dione, 3,4-bis([(3,4-dimethylphenoxy)acetyl]amino)benzoic acid, 2-(5,5-dimethyl-3-methylidenehexyl)-1-methyl-5-(3-adamantylbutyl)-3-propylbenzene, and 2-(3-([((2-[2-(dimethylamino)ethyl]-1H-indol-3-yl)methyl)sulfanyl]methyl)-5-methyl-1H-indol-2-yl)-N,N-dimethylethanamine
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
ACAP3
aGTPase-activating protein (GAP) specific to small GTPase Arf6. ACAP3 is involved in neuronal migration in the developing cerebral cortex of mice, regulation mechanism, detailed overview. ACAP3 is abundantly expressed in the developing cerebral cortex. GAP activity of ACAP3 is required for neuronal migration. Knockdown of ACAP3 in the developing cortical neurons of mice in utero significantly abrogates neuronal migration in the cortical layer, which is restored by ectopic expression of wild-type ACAP3, but not by its GAP-inactive mutant
-
alphabeta-tubulin
soluble alphabeta-tubulin acts as a constitutively active Rheb activator that performs direct Rheb-binding, the deacetylated form has a high binding affinity for Rheb. Deacetylated soluble tubulin has a positive role in Rheb function by increasing the GTP-bound Rheb levels. Overexpression of alpha-tubulin K40A increases Rheb-induced S6K1 phosphorylation
-
CAPRI
-
a member of the GAP1 family of GTPase-activating proteins, GAPs, for small G proteins functioning as an amplitude sensor for intracellular Ca2+ levels stimulated by extracellular signals. It has a catalytic domain with dual Ras-GAP and RapGAP activities, and acts as dimer and monomer. CAPRI switches between its two GAP activities, RasGAP and Rap1GAP, mechanism, overview. Structure and activity of the C-terminal tail of Mus musclus CAPRI, activities on endogenous Rap1 in vivo of the recombinant full-length and C-terminal part of murine CAPRI in CHO cells, overview. Wild-type and monomeric CAPRI translocate to the plasma membrane similarly, but monomers are stronger RasGAPs at the membrane level
-
Epidermal growth factor
stimulates Rac1 as cardiovascular stimulus
exoenzyme S
-
arginine 146 essential for the stimulation of GTPase activity
-
forskolin
-
the adenylyl cyclase activator strongly and specifically activates Rap1 in microvascular smooth muscle cells
geranylgeranyl transferase I
-
RhoA is activated by geranylgeranylation, which promotes its membrane anchoring, the geranylgeranyl transferase I inhibitor GGTI-2166to is used to inhibit geranylgeranylation
-
guanidine nucleotide exchange protein
-
activates. Activated Ras then stimulates Raf, mitogen-activatde protein kinase cascades
-
guanine nucleotide exchange factors
GEF, GTP-binding to small GTPases is catalyzed by GEFs, Trp71 of Rac1 is a critical site for the discrimination of a subset of GEF, including Tiam1 and Trio
-
Insulin-like growth factor
stimulates Rac1 as cardiovascular stimulus
-
interleukin 1beta
stimulates Rac1 as cardiovascular stimulus
-
lipopolysaccharide
Rap2a is activated by lipopolysaccharide in macrophages. In contrast to mRNA levels, Rap2a protein levels are increased after lipopolysaccharide treatments of macrophages
mastoparan
stimulates GTP binding in the presence of Mg2+ and guanine nucleotide exchange, mastoparan mimics the GPCR mode of action
nucleoside diphosphate kinase
-
truncated 12-kDa form, builds complex with Pra with increased GTP and dGTP synthesis activity and decreased CTP and UTP or dCTP and dUTP synthesis activity relative to their synthesis by uncomplexed Ndk
-
platelet-derived growth factor
stimulates Rac1 as cardiovascular stimulus
-
pyruvate kinase
-
builds complex with Pra with specific GTP synthesis activity
Rac
-
activation of Rho, cross-talk between Ras- and Rho subfamilies
-
Sodium fluoride
stimulates of guanine nucleotide exchange, based on the formation of a fluoroaluminate complex which can pass the membrane and occupy the position next to bound GDP and thus stimulates an active state conformation
SOS980-989 peptide
the recombinant SOS980-989 peptide contains the H-Ras-SOScat interaction contact region, which is known to be able to compete with SOScat for binding to H-Ras
-
sphingosine 1 phosphate
stimulates Rac1 as cardiovascular stimulus
T-lymphoma invasion and metastasis factor 1
Tiam1, a GEF, structure analysis in complex with Rac1, specific site of GEF-Rac1 interaction, in particular Trp71
-
Tbc1/cofactor C
acts as a GTPase-activating protein, GAP, in regulating GTPase Alp41/Arl2. Tbc1 and Alp41 directly interact. Tbc1 is the orthologue of cofactor C and is able to form a supercomplex with Alp1D and Alp21E. Temperature-sensitive mutants of tbc1 show loss of microtubules. If Tbc1 loses its GAP activity as in the tbc1-11 mutant, Alp41 will no longer be converted from its active, GTP-bound state to the inactive, GDP-bound state
-
TGF-beta1
TGF-beta1 activates Rap1 through cAMP and Epac1/Epac2. 2',5-dideoxyadenosine is an inhibitor of adenlyate cyclase on Rap1 activity
-
tumor necrosis factor-alpha
stimulates Rac1 as cardiovascular stimulus
-
U46619
-
small GTPase RhoA is activated by the activation of functional receptors for thromboxane A2 like U46619
UNC-73
-
Trio-like guanine nucleotide exchange factor encoded by unc-73, acts as an activator of RHO-1 in the migration process, the UNC-73 GEF2 domain may have the exchange activity on RHO-1 in vivo
-
vascular endothelial growth factor
stimulates Rac1 as cardiovascular stimulus
-
cytotoxic necrotizing factor 1
activation of Rho proteins by the cytotoxic necrotizing factor 1 (CNF1) from Escherichia coli, while the isomeric cytotoxicnecrotizing factor from Yersinia pseudotuberculosis (CNFy) drives GTP-loading of basal RhoB but fails tocause activation of the rhoB promoter and thus its expression. CNF1 inhibits cytokinesis and induces the formation of bi-nucleated (tetraploid) cells. Cytotoxic-necrotizing factors encompass a class of auto-transporter toxins produced by Escherichia coli (CNF1-3) or Yersiniapseudotuberculosis (CNFy). CNF1 deamidates Gln63 in RhoA. CNF1-induced RhoB response depends on the deamidation of Rho proteins
-
cytotoxic necrotizing factor 1
activation of Rho proteins by the cytotoxic necrotizing factor 1 (CNF1) from Escherichia coli, while the isomeric cytotoxicnecrotizing factor from Yersinia pseudotuberculosis (CNFy) drives GTP-loading of basal RhoB but fails to cause activation of the rhoB promoter and thus its expression. CNF1 inhibits cytokinesis and induces the formation of bi-nucleated (tetraploid) cells. Cytotoxic-necrotizing factors encompass a class of auto-transporter toxins produced by Escherichia coli (CNF1-3) or Yersinia pseudotuberculosis (CNFy). CNF1 specifically deamidates RhoA. CNF1-induced RhoB response depends on the deamidation of Rho proteins
-
GTP
the activation state of Rac1 depends on the release of guanosine diphosphate and the binding of guanosine triphosphate. This cycling is regulated by the guanine nucleotide exchange factors, as activators, and by the GTPase activating proteins
GTP
the activation state of Rac1 depends on the release of guanosine diphosphate and the binding of guanosine triphosphate. This cycling is regulated by the guanine nucleotide exchange factors, as activators, and by the GTPase activating proteins. The activation process of Rac1 combines the GDP/GTP switch, catalyzed by GEF and GAP, with a cytosol/membrane alternation, regulated by GDI and protein prenylation, detailed overview
GTP
Rab proteins exist in the active GTP-bound and inactive GDP-bound conformations with the GTP/GDP exchange mediated by GTP exchange factors (GEF53) and it is the GTP-bound active form of Rab that promotes membrane trafficking upon interaction with effector proteins
GTPase activating protein GAP
-
for Ras-related proteins, stimulates intrinsic GTPase reaction
-
GTPase activating protein GAP
-
p190, binding to and activation of RhoA and cdc42
-
GTPase activating protein GAP
-
Rap-GAP in neutrophil cytosol, increased rate of GTP hydrolysis
-
GTPase activating protein GAP
-
Rap2-GAP, stimulation of both Rap1 and Rap2 proteins
-
GTPase activating protein GAP
-
complex formation with Ran, stimulates intrinsic GTPase activity
-
GTPase activating protein GAP
-
for Ras-related proteins, stimulates intrinsic GTPase reaction
-
GTPase activating protein GAP
-
stimulating intrinsic GTPase acitivity
-
GTPase activating protein GAP
-
for Ras-related proteins, stimulates intrinsic GTPase reaction
-
GTPase activating protein GAP
-
Gyp1p, Gyp7p, specificity for Ypt/Rab GTPases, enhancement of intrinsic GTP hydrolysis rate
-
GTPase activating protein GAP
-
stimulating intrinsic GTPase acitivity
-
GTPase activating protein GAP
-
complex formation with Ran, stimulates intrinsic GTPase activity
-
guanine nucleotide exchange factor
-
Ypt1p requires guanine nucleotide exchange factor for the GDP-GTP exchange and subsequent activation of the signaling process
-
guanine nucleotide exchange factor Epac
-
specifically increases Rap1 activity
-
guanine nucleotide exchange factor Epac
-
specifically increases Rap1 activity
-
guanine nucleotide exchange factor GEF
-
activation of RhoGTPases through direct protein-protein interaction
-
guanine nucleotide exchange factor GEF
-
facilitates loading with GTP
-
guanine nucleotide exchange factor GEF
-
activation of RhoGTPases through direct protein-protein interaction
-
heparin-binding epidermal growth factor-like growth factor
-
induces rapid and strong RhoA activation
-
heparin-binding epidermal growth factor-like growth factor
-
induces rapid and strong RhoA activation
-
Insulin
-
RalA is activated upon insulin stimulation in a dose-dependent manner
-
lysophosphatidic acid
stimulates Rac1 as cardiovascular stimulus
lysophosphatidic acid
-
activation of Rho, assembly of contractile actin-myosin filaments and focal adhesion complexes
Rac-specific GEF Tiam1
activates Rac3, but less efficiently than the Rac isoform Rac2
-
Rac-specific GEF Tiam1
stimulates the GDP exchange reaction, increases the GDP dissociation rate, activates Rac1 less efficiently than Rac2
-
Rac-specific GEF Tiam1
stimulates the GDP exchange reaction, increases the GDP dissociation rate, activates Rac2 more efficiently than the Rac isoforms Rac1 and Rac3
-
additional information
-
exposure of confluent lung endothelial cell monolayers to wild type Pseudomonase aeruginosa strain PAK causes a significant increase in RhoA activity within 10 min
-
additional information
the recruited CFP-tagged RhoA on the parasitophorous vacuole membrane cannot be activated by epithelial growth factor and no translocation is observed, unlike the unassociated RhoA in the host cell cytosol that migrates to the cell membrane towards the epithelial growth factor activation spot
-
additional information
the recruited CFP-tagged RhoA on the parasitophorous vacuole membrane cannot be activated by epithelial growth factor and no translocation is observed, unlike the unassociated RhoA in the host cell cytosol that migrates to the cell membrane towards the epithelial growth factor activation spot
-
additional information