Any feedback?
Please rate this page
(all_enzymes.php)
(0/150)

BRENDA support

3.6.5.2: small monomeric GTPase

This is an abbreviated version!
For detailed information about small monomeric GTPase, go to the full flat file.

Word Map on EC 3.6.5.2

Reaction

GTP
+
H2O
=
GDP
 +
phosphate

Synonyms

ADP-ribosylation factor 6, ADP-ribosylation factor-like protein 2, Alp41, Alp41/Arl2, ARD1, Arf 1, Arf 1-6, Arf-like 3 small GTPase, Arf6, ARL2, Arl6, Arl6/BBS3, Arl9, AtRopGEF12, Cdc42, Cdc42Hs, Der, Der GTPase, double Era-like protein, EC 3.6.1.47, EF-Tu, EhRab11B, elF-2, EmRas, FgCdc42, FgRac1, FgRHO1, FgRHO2, FgRHO3, FgRHO4, GCC185, Gem, GhRac1 GTPase, Gsp1p, GTP-phosphohydrolase, GTPase, GTPase Alp41/Arl2, GTPase TcRho1, GTPase Toc33, GTPase Toc33/34, guanine triphosphatase, guanosine 5'-triphosphatase, guanosine triphosphatase, H-Ras, K-Ras, Kir, Krev-1, M-Ras, monomeric G protein, monomeric GTPase, More, non-canonical Ras-like G protein, OsRac1, p21 ras, Pc-Rac1, PfG, PRA, Pra2, Pra3, Rab GTPase, Rab GTPase protein 5, Rab11, Rab13, Rab15, Rab18, Rab1a, Rab1B, Rab21, Rab23, Rab27a, Rab27a GTPase, Rab27B, Rab2A, Rab2B, Rab30, Rab33A, Rab35, Rab36, Rab37, Rab38, Rab3A, Rab4a, Rab6A, Rab6B, Rab8, Rab8A, Rab9A, Rab9B, RabE, RabE1d, Rac, Rac GTPase, Rac-like GTP-binding protein 1, Rac1, Rac1 GTPase, Rac2, Rac3, Rac4, Rad, Rad GTPase, Ral GTPase, RalA, RalB, Ran, RAP, Rap GTPase, Rap1, Rap1 small GTPase, Rap1A, Rap1b, Rap2, Rap2 small GTPase, Rap2a, Rap2C, RAS, Ras GTPase, Ras homolog enriched in brain-like protein 1, Ras proximity 1, Ras related GTPase Rap, Ras-associated protein 1, Ras-like G-protein, Ras-like GTpase, Ras-related C3 botulinum toxin substrate 1, Ras-related protein rab-5, putative, Ras-related small GTPase, RAS1, RAS2, RasL10B, Rasl11a, Rem2, Rhb1, Rheb, Rheb GTPase, RHEBL1, Rho, Rho family small GTPase, Rho GTPase, RHO-1, Rho-GTPase, Rho-type GTPase, Rho-type small GTPase, Rho1, Rho1p, Rho3, Rho3p, RhoA, rhoA p21, RhoB, rhoB p20, RhoC, RhoGTPase, RhoH, ribosomal GTPase, ribosome-small-subunit-dependent GTPase A, RsgA, Ryh1, Ryh1 GTPase, Sar1, SdArf1, SdArf1-like, SdArf10, SdArf5, SdArf6, SdArl1, SdCdc42, SdK-Ras2, SdRab-like1, SdRab-like2, SdRab-like3, SdRab-like4, SdRab-like5, SdRab-like6, SdRab1-like, SdRab10, SdRab11, SdRab14, SdRab18, SdRab2, SdRab20-like, SdRab21, SdRab21-like, SdRab24, SdRab28, SdRab3, SdRab32, SdRab35, SdRab39, SdRab4, SdRab41/43, SdRab5, SdRab8, SdRac, SdRalA, SdRan, SdRap1, SdRap1-like, SdRheb, SdRho1, SdRho2, SdRho3, small G protein, small GTPase, small GTPase ARF6, small GTPase LIP1, small GTPase protein Rac-1, small GTPase Rab1, small GTPase Rab11b, small GTPase Rab2, small GTPase Rab21, small GTPase Rab27b, small GTPase Rac, small GTPase Rac-1, small GTPase Ral, small GTPase Ras, small GTPase Ras-related protein in brain 13, small GTPase Rho, small GTPase RhoA, small GTPase RhoV, small GTPase Rnd1, small GTPases Rab5, small GTPases Ral5, small nuclear GTPase Ran, small Rho GTPase, small Rho GTPase Rac1, small, monomeric G protein, small-GTPase, SmGTP, TbArl6, TcRABL4, vacuolar Rab GTPase, Wrch-1, YjeQ, Ypt1, Ypt1p, Ypt7, Ypt7p, YsxC

ECTree

     3 Hydrolases
         3.6 Acting on acid anhydrides
             3.6.5 Acting on GTP to facilitate cellular and subcellular movement
                3.6.5.2 small monomeric GTPase

Inhibitors

Inhibitors on EC 3.6.5.2 - small monomeric GTPase

Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
INHIBITOR
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
-
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
-
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
CCG-1423
-
-
CCG-977
-
-
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
Clostridium botulinum exoenzyme C3
-
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
-
binding of GTP completely abolished
GTPase activating protein
-
-
-
GTPgammaS
-
Arl6 is competitively inhibited by the increasing concentrations of non-radioactive GTPgammaS
guanine nucleotide dissociation inhibitor GDI
-
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-acetylphenyl)-4-([2-(4-chloro-2-methylphenoxy)propanoyl]amino)benzamide
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
NSC23766
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
-
Rap1GAP1
-
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
-
additional information
-