Information on EC 3.6.5.2 - small monomeric GTPase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY hide
3.6.5.2
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RECOMMENDED NAME
GeneOntology No.
small monomeric GTPase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
GTP + H2O = GDP + phosphate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphorous acid anhydride hydrolysis
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PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
NIL
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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).
CAS REGISTRY NUMBER
COMMENTARY hide
9059-32-9
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
strain SC5314
UniProt
Manually annotated by BRENDA team
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SwissProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
strain A19
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Manually annotated by BRENDA team
EF-Tu
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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SwissProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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UniProt
Manually annotated by BRENDA team
diverse genes encoding fourteen PpRAB, seven PpARF/ARL/SAR, two PpROP and one PpRAN GTPases, overview
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Manually annotated by BRENDA team
strain 8830
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Manually annotated by BRENDA team
strain 8830
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Manually annotated by BRENDA team
gene alp41
UniProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
GTP + H2O
GDP + phosphate
show the reaction diagram
guanosine 5'-O-(3-thio)triphosphate + H2O
guanosine 5'-diphosphate + thiophosphate
show the reaction diagram
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?
guanosine 5'-O-(3-thiotriphosphate) + H2O
guanosine 5'-O-diphosphate + thiophosphate
show the reaction diagram
MEK kinase 1 + H2O
?
show the reaction diagram
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RhoA binds and activates MEK kinase 1
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?
p21-activated kinase 1 + H2O
activated p21-activated kinase 1 + ?
show the reaction diagram
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Gamide signals Rac/Cdc42 to activate p21-activated kinase 1
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?
Rho-activated kinase + H2O
activated Rho-activated kinase + ?
show the reaction diagram
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Ggly signals Rac/Cdc42 to activate Rho-activated kinase
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?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
GTP + H2O
GDP + phosphate
show the reaction diagram
p21-activated kinase 1 + H2O
activated p21-activated kinase 1 + ?
show the reaction diagram
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Gamide signals Rac/Cdc42 to activate p21-activated kinase 1
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?
Rho-activated kinase + H2O
activated Rho-activated kinase + ?
show the reaction diagram
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Ggly signals Rac/Cdc42 to activate Rho-activated kinase
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?
additional information
?
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
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activates
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
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'-p-fluorosulfonylbenzoylguanosine
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irreversible substrate analogue-binding
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
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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
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binding of calmodulin to GST-immobilized Kir/Gem peptide inhibits GTP binding
CCG-1423
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CCG-977
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cerivastatin
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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
Clostridium botulinum exoenzyme C3
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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
ethylenediaminetetraacetic acid
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binding of GTP completely abolished
GTPase activating protein
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GTPgammaS
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Arl6 is competitively inhibited by the increasing concentrations of non-radioactive GTPgammaS
guanine nucleotide dissociation inhibitor GDI
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lovastatin
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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-acetylphenyl)-4-([2-(4-chloro-2-methylphenoxy)propanoyl]amino)benzamide
N-(2-chlorobenzyl)-N-[[(4-methylphenyl)sulfonyl]carbamoyl]-L-alanine
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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
NSC23766
p21 activated kinase
PAK, inhibits nucleotide dissociation from enzyme; PAK, inhibits nucleotide dissociation from enzyme
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Rap1Gap
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the GTPase activating protein catalyzes the hydrolysis of GTP by its asparagine side chain rendering Rap1 inactive
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Rap1GAP1
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simvastatin
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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
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Yersinia outer protein T
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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
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additional information
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