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3.4.17.21: Glutamate carboxypeptidase II

This is an abbreviated version!
For detailed information about Glutamate carboxypeptidase II, go to the full flat file.

Word Map on EC 3.4.17.21

Reaction

release of an unsubstituted, C-terminal glutamyl residue, typically from Ac-Asp-Glu or folylpoly-gamma-glutamates =

Synonyms

100 kDa ileum brush border membrane protein, Acetylaspartylglutamate dipeptidase, altered meristem program1, AMP1, Dipeptidase, acetylaspartylglutamate, EC 3.4.19.8, FGCP, folate hydrolase, folate hydrolase 1, FOLH1, Folylpoly-gamma-glutamate carboxypeptidase, folylpoly-gamma-glutamate carboxypeptidase II, GCP II, GCPII, GCPIII, glutamate carboxypeptidase, glutamate carboxypeptidase II, glutamate carboxypeptidase III, GPCPII, I100, Ileal dipeptidylpeptidase, Membrane glutamate carboxypeptidase, mGCP, More, N-acetyl-alpha-linked acidic dipeptidase, N-acetyl-alpha-linked acidic dipeptidase I, N-acetylaspartylglutamate peptidase, N-acetylated alpha-linked acid dipeptidase, N-Acetylated alpha-linked acidic dipeptidase, N-Acetylated-alpha-linked acidic dipeptidase, N-acetylated-alpha-linked acidic dipeptidase 2, N-acetylated-alpha-linked acidic dipeptidase II, N-Acetylated-alpha-linked-acidic dipeptidase, N-acetylated-alpha-linked-acidic-dipeptidase, N-Acetylated-alpha-linked-amino dipeptidase, NAADLADase, NAADLADse, NAAG degradation enzyme, NAAG peptidase, NAAG peptidase II, NAAG-hydrolyzing activity, NAALA dipeptidase, NAALADase, Naaladase I, NAALADase II, NLD I, PMSA, prostate specific membrane antigen, Prostate-specific membrane antigen, Prostate-specific membrane antigen homolog, prostate-specificmembrane antigen, Prostrate-specific membrane antigen, PSM, PSM antigen, PSMA, Pteroylpoly-gamma-glutamate carboxypeptidase, Rat NAAG peptidase

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.17 Metallocarboxypeptidases
                3.4.17.21 Glutamate carboxypeptidase II

Inhibitors

Inhibitors on EC 3.4.17.21 - Glutamate carboxypeptidase II

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2S)-2-([hydroxy[2-(4-hydroxyphenyl)ethoxy]phosphoryl]methyl)pentanedioic acid
-
-
(2S)-2-([[2-(4-fluorophenyl)ethoxy](hydroxy)phosphoryl]methyl)pentanedioic acid
-
-
(2S)-2-([[2-(4-[[N-(tert-butoxycarbonyl)glycyl]amino]phenyl)ethoxy](hydroxy)phosphoryl]methyl)pentanedioic acid
-
-
(2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid
(2S)-2-[([[(1S)-1,3-dicarboxypropyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]carbonyl)amino]pentanedioic acid
-
the inhibitor has the ability to reduce the perception of inflammatory pain
(2S)-2-[([[(1S)-1-carboxy-2-phenylethyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(1S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(1S)-1-carboxy-3-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]-4-(2H-tetrazol-5-yl)butanoic acid
-
-
(2S)-2-[([[(1S)-3-carboxy-1-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[([[(S)-carboxy(4-hydroxyphenyl)methyl]amino]carbonyl)amino]pentanedioic acid
-
-
(2S)-2-[[(2-[4-[(tert-butoxycarbonyl)amino]phenyl]ethoxy)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S)-2-[[([(1S)-1-carboxy-3-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl]amino)carbonyl]amino]pentanedioic acid
-
-
(2S)-2-[[([(1S)-3-carboxy-1-[2-(2-cyanoethyl)-2H-tetrazol-5-yl]propyl]amino)carbonyl]amino]pentanedioic acid
-
-
(2S)-2-[[butyl(hydroxy)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[ethyl(hydroxy)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[hydroxy(2-phenylethoxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S)-2-[[hydroxy(3-phenylpropoxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S)-2-[[hydroxy(methyl)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[hydroxy(phenyl)phosphorothioyl]amino]pentanedioic acid
-
-
(2S)-2-[[hydroxy(phenyl)phosphorothioyl]oxy]pentanedioic acid
-
-
(2S)-2-[[hydroxy(phenyl)phosphoryl]amino]pentanedioic acid
-
-
(2S)-2-[[[2-[4-(acetylamino)phenyl]ethoxy](hydroxy)phosphoryl]methyl]pentanedioic acid
-
-
(2S,2'S,4R)-4-benzyl-N,N'-carbonyldiglutamic acid
-
-
(2S,2'S,4R,4'R)-4,4'-dibenzyl-N,N'-carbonyldiglutamic acid
-
-
(2S,2'S,4R,4'R)-N,N'-carbonyl-4,4'-dimethyldiglutamic acid
-
-
(2S,2'S,4S)-N,N'-carbonyl-4-methyldiglutamic acid
-
-
(2S,2'S,4S,4'S)-N,N'-carbonyl-4,4'-dimethyldiglutamic acid
-
-
(2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid
-
EPE, a phosphapeptide transition state analog of glutamyl-glutamate
(2S,4R)-2-[([[(1S,3R)-1,3-dicarboxybutyl]amino]carbonyl)amino]-4-methylpentanedioic acid
-
-
(2S,4S)-2-[([[(1S,3S)-1,3-dicarboxybutyl]amino]carbonyl)amino]-4-methylpentanedioic acid
-
-
(4S)-4-[([[(1S)-3-carboxy-1-(2H-tetrazol-5-yl)propyl]amino]carbonyl)amino]-4-(2H-tetrazol-5-yl)butanoic acid
-
-
(9S,13S)-1-(3-iodophenyl)-3,11-dioxo-2,4,10,12-tetraazapentadecane-9,13,15-tricarboxylic acid
-
-
(R)-2-(3-mercaptopropyl)-pentanedioic acid
(R)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
(R)-2-(phosphonomethyl)-pentanedioic acid
(S)-2-(3-((R)-1-carboxy-(2-methylthio)ethyl)ureido)pentanedioic acid
DCMC
(S)-2-(3-((R)-1-carboxy-2-(4-fluorobenzylthio)ethyl)ureido)pentanedioic acid
DCFBC
(S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid
(S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid
(S)-2-(3-((S)-1-carboxy-5-(1,2-dicarba-closo-dodecarboranylamido) pentyl)ureido)pentanedioic acid
-
(S)-2-(3-((S)-1-carboxy-5-(2-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(2-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-bromophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-chlorophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-fluorophenyl)ureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-(4-iodophenyl)ureido)pentyl)ureido)pentanedioic acid
(S)-2-(3-((S)-1-carboxy-5-(3-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(3-phenylureido)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-bromobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-chlorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-fluorobenzylamino)pentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-iodobenzylamino)pentyl)ureido)-pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(4-iodobenzylamino)pentyl)ureido)pentanedioic acid
-
i.e. MIP-1072, the compound shows affinity to and uptake into prostate cancer cells, binding analysis, overview
(S)-2-(3-((S)-1-carboxy-5-(4-iodophenylsulfonamido)pentyl)-ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-1-carboxy-5-(naphthalen-1-ylmethylamino)pentyl)-ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-5-(6-(4-(4-(4-acetylpiperazin-1-yl)phenyl)piperazin-1-yl)-N-(4-bromobenzyl)nicotinamido)-1-carboxypentyl)ureido)-pentanedioic acid
4200fold selectivity compared to glutamate carboxypeptidase III
(S)-2-(3-((S)-5-(6-(4-(4-(4-acetylpiperazin-1-yl)phenyl)piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid
1400fold selectivity compared to glutamate carboxypeptidase III
(S)-2-(3-((S)-5-(benzylamino)-1-carboxypentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-((S)-5-(N-(4-bromobenzyl)-6-(4-(4-(4-(4-carboxy-3-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoyl)piperazin-1-yl)phenyl)-piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid
1900fold selectivity compared to glutamate carboxypeptidase III
(S)-2-(3-((S)-5-(N-(4-bromobenzyl)-6-(4-(4-(4-(41-oxo-45-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10,13,16,19,22,25,28,31,34,37-dodecaoxa-40-azapentatetracontan-1-oyl)piperazin-1-yl)phenyl)piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid
6600fold selectivity compared to glutamate carboxypeptidase III
(S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido)pentanedioic acid
-
-
(S)-2-(3-(4-iodobenzyl)ureido)pentanedioic acid
-
-
(S)-2-(3-mercaptopropyl)-pentanedioic acid
(S)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
(S)-2-(phosphonomethyl)-pentanedioic acid
(S)-2-[3-((S)-1-carboxy-2-(4-hydroxyphenyl)ethyl)ureido]pentanedioic acid
(S)-2-[3-((S)-1-carboxy-2-phenylethyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-1-carboxy-3-(1H-tetrazol-5-yl)propyl)ureido]pentanedioic acid
(S)-2-[3-((S)-1-carboxy-3-(methylsulfanyl)propyl)ureido]pentanedioic acid
(S)-2-[3-((S)-1-carboxy-3-methylbutyl)ureido]pentanedioic acid
(S)-2-[3-((S)-1-carboxy-3-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-3-carboxy-1-(1H-tetrazol-5-yl)propyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-3-carboxy-1-[1-(2-cyanoethyl)-1H-tetrazol-5-yl]propyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-alpha-carboxy-4-hydroxybenzyl)ureido]pentanedioic acid
-
-
(S)-2-[3-((S)-alpha-carboxybenzyl)ureido]pentanedioic acid
-
-
(S)-2-[3-(S)-(1,3-dicarboxypropyl)ureido]pentanedioinc acid
(S)-alpha-ethylglutamate
-
specific group II metabotropic glutamate receptor antagonist, in vivo activity
(S,S)-4,4'-bis[1-(2-cyanoethyl)-1H-tetrazol-5-yl]-2,2'-ureylenedibutyric acid
-
-
(S,S)-4,4'-bis[1-(2-cyanoethyl)-1H-tetrazol-5-yl]-4,4'-ureylenedibutyric acid
-
-
(S,S)-4,4'-di-(1H-tetrazol-5-yl)-2,2'-ureylenedibutyric acid
-
-
(S,S)-4,4'-di-(1H-tetrazol-5-yl)-4,4'-ureylenedibutyric acid
-
-
(S,S)-N,N'-carbonyl-2,2'-dimethyldiglutamic acid
-
-
(t-Bu)Cys-PSI[C-O]-Glu
-
IC50: 29 nM
(Z)-N-(N-Acetyldehydroaspartyl)-L-Glu
-
-
1,10-phenanthroline
-
1 mM, 90% inhibition
2-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 1700 nM
2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid
-
IC50: 2200 nM
2-(3-carboxybenyl)succinic acid
-
IC50: 0.015 mM
2-(3-cyanobenzyl)-5-mercaptopentanoic acid
-
IC50: 1800 nM
2-(3-hydroxybenzyl)-3-phosphonopropanoic acid
-
IC50: 508 nM
2-(3-mercaptopropyl)-pentanedioic acid
2-(3-mercaptopropyl)pentanedioic acid
2-(3-sulfanylpropyl)pentanedioic acid
-
i.e. GPI-5693, attenuates cocaine-induced conditioned place preference
2-(phosphonomethyl) pentanedioic acid
inhibitor completely blocks N-acetylaspartylglutamate cleavage activity but not Amyloid-beta degradation
2-(phosphonomethyl)-4-(5H-tetrazol-5-yl)butanoic acid
-
IC50: 175 nM
2-(phosphonomethyl)-pentanedioic acid
2-(phosphonomethyl)hexanedioic acid
-
IC50: 185 nM
2-(phosphonomethyl)hexanoic acid
-
IC50: 185 nM
2-(phosphonomethyl)pentandioic acid
10fold selectivity compared to glutamate carboxypeptidase III
2-(phosphonomethyl)pentanedioic acid
2-(Phosphonomethyl)pentanoate
-
-
2-(phosphonomethyl)succinic acid
-
IC50: 2200 nM
2-([hydroxy[3-(trifluoromethyl)benzyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 55 nM
2-([hydroxy[hydroxy(phenyl)methyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 55 nM
2-([hydroxy[hydroxy(pyridin-4-yl)methyl]phosphoryl]methyl)pentanedioic acid
-
IC50: 10 nM
2-amino-3-(3,5-dioxo[1,2,4]oxadiazolidin-2-yl)propionic acid
-
i.e. quisqualic acid, a glutamate-like inhibitor of GCPIII and GCPII
2-benzyl-3-phosphonopropanoic acid
-
IC50: 548 nM
2-benzyl-5-mercaptopentanoic acid
-
IC50: 1400 nM
2-oxoglutarate
-
0.1 mM, 46% inhibition
2-phosphonomethyl-pentanedoic acid
-
2-PMPA
2-[(hydroxy[[(4-methoxyphenyl)amino]methyl]phosphoryl)methyl]pentanedioic acid
-
IC50: 3 nM
2-[[(2,4-dicarboxybutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 0.5 nM
2-[[(2-carboxy-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 2 nM
2-[[(2-carboxy-4-phenylbutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 2 nM
2-[[(2-carboxyethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 1 nM
2-[[(2-carboxypropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 1.5 nM
2-[[(2-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 156 nM
2-[[(3,5-difluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 49 nM
2-[[(3-aminobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 143 nM
2-[[(3-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 70 nM
2-[[(4-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 64 nM
2-[[(anilinomethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 4 nM
2-[[benzyl(hydroxy)phosphoryl]methyl]pentanedioic acid
2-[[hydroxy(2-phenylethyl)phosphoryl]methyl]pentanedioic acid
2-[[hydroxy(3-nitrobenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50 59 nM
2-[[hydroxy(3-phenylpropyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 230 nM
2-[[hydroxy(4-methoxybenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 90 nM
2-[[hydroxy(4-methylbenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 68 nM
2-[[hydroxy(pentafluorobenzyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 82 nM. Significantly prevents neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In the chronic constrictive model of neuropathic pain, the inhibitor sifnificantly attenuats the hypersensitivity observed with saline-treated animals
2-[[hydroxy(phenyl)phosphoryl]methyl]pentanedioic acid
-
IC50: 2930 nM
2-[[hydroxy(propyl)phosphoryl]methyl]pentanedioic acid
2-[[[(3-fluorophenyl)(hydroxy)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 16 nM
2-[[[(benzylamino)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 59 nM
2-[[[3,5-bis(trifluoromethyl)benzyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 55 nM
2-[[[3-(benzyloxy)-2-methyl-3-oxopropyl](hydroxy)phosphoryl]methyl]pentanedioic acid
-
IC50: 95 nM
2-{[2-Carboxy-3-(4-methoxy-phenylamino)-propyl]-hydroxy-phosphinoylmethyl}-pentanedioic acid
-
IC50: 3 nM
3-(1-carboxy-4-mercaptobutoxy)benzoic acid
-
IC50: 14 nM
3-(2-carbamoyl-5-mercaptopentyl)benzoic acid
-
IC50: 640 nM
3-(2-carboxy-3-hydroxycarbamoylpropyl)benzoic acid
-
IC50: 0.015 mM
3-(2-carboxy-3-phosphonopropyl)benzoic acid
-
IC50: 120 nM
3-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 15 nM
3-(2-carboxy-5-mercaptopentyl)benzoic acid methyl ester
-
IC50: 2700 nM
3-(2-carboxy-5-mercaptosulfanylpentyl)benzoic acid
-
IC50: 0.02 mM
3-(2-carboxy-5-tritylsulfanylpentyl)benzoic acid
-
IC50: 0.02 mM
3-(2-oxotetrahydro-thiopyran-3-yl)propionic acid
-
prodrug of inhibitor 2-(3-mercaptopropyl)pentanedioic acid
3-(3-mercaptopropyl)pentanedioic acid
-
presynaptic action of enzyme inhibition, enzyme inhibition depresses mossy fiber-CA3 synaptic transmission
3-(5-mercapto-2-methoxycarbonylpentyl)benzoic acid
-
IC50: 730 nM
3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid
-
IC50: 32 nM
3-[2-carboxy-3-(hydroxypentafluorophenylmethylphosphinoyl)propyl]benzoic acid
-
IC50: 2400 nM
4,4'-phosphinicobis(butane-1,3-dicarboxylic acid)
4-(2-carboxy-5-mercaptopentyl)benzoic acid
-
IC50: 63 nM
4-(3-hydroxyphenyl)-2-(phosphonomethyl)butanoic acid
-
IC50: 508 nM
4-cyano-2-(phosphonomethyl)butanoic acid
-
IC50: 335 nM
4-phenyl-2-(phosphonomethyl)butanoic acid
-
IC50: 199 nM
4-[(2-(R))-2-carboxy-5-(oxidanylamino)-5-oxidanylidene-pentyl]benzoic acid
-
4-[(2-(S))-2-carboxy-5-(oxidanylamino)-5-oxidanylidene-pentyl]benzoic acid
-
4-[[bis[[(isopropoxycarbonyl)oxy]methoxy]phosphoryl]-methyl]-5-[[(isopropoxycarbonyl)oxy]methoxy]-5-oxopentanoic acid
5-oxoheptane-1,3,7-tricarboxylic acid
-
0.1 mM, 35% inhibition
5-oxononane-1,3,7,9-tetracarboxylic acid
-
inhibitor possesses mGluR3 agonist activity
Ala-Glu
-
0.0061 mM, 50% inhibition
Asp-Ala
-
0.1 mM, 26% inhibition
Asp-Asp
-
0.1 mM, 42% inhibition
Asp-Glu
Asp-Phe
-
0.1 mM, 22% inhibition
Asp-PSI[C-O-S]-Glu
-
IC50: 0.0461 mM
Asp-PSI[C-O]-Asp
-
IC50: 0.0038 mM
Asp-PSI[S]-Asp
-
0.1 mM, 42% inhibition
aspartate
-
0.1 mM, 42% inhibition
bestatin
-
0.29 mM, 79% inhibition
Cys-PSI[C-O-S]-Glu
-
IC50: 6.9 nM
cysteate
-
0.1 mM, 40% inhibition
cysteine sulfinate
-
0.1 mM, 42% inhibition
D-Glu-D-Glu
-
0.1 mM, 50% inhibition
D-Glu-PSI[C-O]-D-Glu
-
0.1 mM, 67% inhibition
D-Glu-PSI[C-O]-Glu
-
0.001 mM, 25% inhibition
diazabicycloalkane
-
diphenyl 2-[[[2-[4-([[7-(diethylamino)-2-oxo-2H-chromen-3-yl]carbamoyl]amino)phenyl]ethoxy](hydroxy)phosphoryl]methyl]pentanedioate
-
-
dithiothreitol
-
1 mM, 94.8% inhibition
DKFZ-PSMA-11
720fold selectivity compared to glutamate carboxypeptidase III
DUPA
-
enzyme active site binding structure, docking and modelling, detailed overview
gamma-Glu-Glu
Glu-Asp
-
0.1 mM, 27% inhibition
Glu-Glu
Glu-Glu-Glu
Glu-PSI[C-O-C-O]-Glu
-
0.001 mM, 9% inhibition
Glu-PSI[C-O]-Glu
-
IC50: 47 nM
glutathione
-
i.e. gamma-Glu-Cys-Gly, 0.019 mM, 50% inhibition
Gly-Glu
Gly-Gly-Glu
-
0.00098 mM, 50% inhibition
Gly-PSI[C-O-S]-Glu
-
0.001 mM, 46% inhibition
GPI 5693
-
i.e. (R,S)-2-(3-mercaptopropyl)-pentanedioic acid or 2-MPPA, pharmacokinetics and safety of the NAALADase-inhibitor and its effects on the central nervous system after application in vivo, overview
GPI-16476
-
enantiomer of GPI-5693
GPI-16477
-
enantiomer of GPI-5693
GPI-18431
-
enzyme active site binding structure, docking and modelling, detailed overview
GPI-5693
-
-
GPI5232
Ibotenate
-
0.1 mM, 45% inhibition
iodoacetate
-
1 mM, 38% inhibition
L-2-Amino-4-phosphonobutanoate
-
0.1 mM, 37% inhibition
L-Glu
LY341495
-
-
MOPS
-
-
N-(3,4-Dicarboxybutanoyl)glutamic acid
-
-
N-(4-fluorobenzoyl)-L-isoleucyl-O-[[[(1S)-1,3-dicarboxypropyl]amino](hydroxy)phosphoryl]-L-serine
-
N-(4-fluorobenzoyl)-L-valyl-O-[[[(1S)-1,3-dicarboxypropyl]amino](hydroxy)phosphoryl]-L-serine
-
N-(Dicarboxymethyl)acetylglutaminic acid
-
-
N-(tert-butoxycarbonyl)glycyl-N-[4-[2-([[(2S)-2,4-dicarboxybutyl](hydroxy)phosphoryl]oxy)ethyl]phenyl]-L-prolinamide
-
-
N-(tert-butoxycarbonyl)glycylglycyl-N-[4-[2-([[(2S)-2,4-dicarboxybutyl](hydroxy)phosphoryl]oxy)ethyl]phenyl]glycinamide
-
-
N-([(1S)-1-carboxy-5-([(4-iodophenyl)carbonyl]amino)pentyl]carbamoyl)-L-glutamic acid
P1'-diversified urea-based inhibitor, in complex with enzyme PDB entry 3D7H
N-2-([(1S)-1-carboxy-2-(furan-2-yl)ethyl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine
P1'-diversified urea-based inhibitor, in complex with enzyme PDB entry 4OC3
N-2-([(1S)-1-carboxybut-3-yn-1-yl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine
P1'-diversified urea-based inhibitor, in complex with enzyme PDB entry 4OC2
N-Acetyl-Asp-Gln
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0.1 mM, 49% inhibition
N-Acetyl-Asp-Glu-Asp
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0.1 mM, 49% inhibition
N-Acetyl-Asp-Ser-Gly
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0.1 mM, 37% inhibition
N-Acetyl-beta-L-Asp-L-Glu
N-Acetyl-Glu-Asp
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0.036 mM, 50% inhibition
N-Acetyl-Glu-Glu
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0.00031 mM, 50% inhibition
N-acetyl-L-Asp
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0.1 mM, 38% inhibition
N-Acetyl-L-Asp-L-Glu
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0.00054 mM, 50% inhibition
N-acetyl-L-Glu
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0.058 mM, 50% inhibition
N-Fumaryl-L-Glu
-
-
N-Succinyl-L-Glu
-
-
N-[(2-benzamidoethoxy)(hydroxy)phosphoryl]-L-glutamic acid
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N-[4-carboxy-3-(carboxymethyl)-3-hydroxybutanoyl]-L-glutamic acid
N-[hydroxy(4-phenylbutoxy)phosphoryl]-L-glutamic acid
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N-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]-L-glutamic acid
N-[[(1S)-1-carboxy-3-(methylsulfanyl)propyl]carbamoyl]-L-glutamic acid
N-[[(1S)-1-carboxy-3-methylbutyl]carbamoyl]-L-glutamic acid
N-[[(1S)-1-carboxy-5-(4-iodobenzamido)pentyl]carbamoyl]-L-glutamic acid
N-[[(1S)-1-carboxy-5-([5-[3-(3-[[[2-[[[5-(2-carboxyethyl)-2-hydroxyphenyl]methyl](carboxymethyl)amino]ethyl](carboxymethyl)amino]methyl]-4-hydroxyphenyl)propanamido]pentanoyl]amino)pentyl]carbamoyl]-L-glutamic acid
N-[[(1S)-5-([(4-bromophenyl)methyl][6-[4-(4-[4-[4-carboxy-3-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoyl]piperazin-1-yl]phenyl)piperazin-1-yl]pyridine-3-carbony]amino)-1-carboxypentyl]carbamoyl]-L-glutamic acid
N-[[(1S)-5-acetamido-1-carboxypentyl]carbamoyl]-L-glutamic acid
N-[[(1S)-5-[acetyl[(4-bromophenyl)methyl]amino]-1-carboxypentyl]carbamoyl]-L-glutamic acid
N-[[(2R)-2-benzamido-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
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N-[[(2S)-2-benzamido-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
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N-[[(2S)-2-[[(6S)-6-amino-6-carboxy-3-oxohexyl]amino]-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
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N-[[([1,1'-biphenyl]-4-yl)methoxy](hydroxy)phosphoryl]-L-glutamic acid
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N-[[[(1S)-1-carboxy-3-methylbutyl]amino]carbonyl]-L-glutamic acid
i.e. ZJ-43. 160fold selectivity compared to glutamate carboxypeptidase III
Phe-Glu
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0.077 mM, 50% inhibition
pteroylglutamic acid
-
-
puromycin
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0.5 mM, 55% inhibition
pyroglutamate
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0.1 mM, 27% inhibition
pyropheophorbide-a conjugate
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i.e. Ppa-2 conjugate, non-specificity of unconjugated Ppa, conjugation of a peptidomimetic inhibitor of PSMA to the porphyrinic PS, pyropheophorbide-a gives
quinolinate
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0.1 mM, 41% inhibition
Quisqualic acid
S-2-((2-(S-4-(4-18F-fluorobenzamido)-4-carboxybutanamido)-S-2-carboxyethoxy)hydroxyphosphorylamino)-pentanedioic acid
-
-
S-2-((2-(S-4-amino-4-carboxybutanamido)-S-2-carboxyethoxy)-hydroxyphosphorylamino)-pentanedioic acid
-
phosphoramidate
Serine O-sulfate
-
0.042 mM, 50% inhibition
t-BuNHC(O)-Glu
-
0.001 mM, 10% inhibition
Tyr-Glu
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0.1 mM, 45% inhibition
VA-033
Val-Glu-Glu
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0.036 mM, 50% inhibition
ZJ-43
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i.e. (S)-2-[3-((S)-1-carboxy-3-methylbutyl)ureido]pentanedioic acid, the inhibitor enhances extracellular NAAG levels and reduces extracellular levels of amino acids neurotransmitter following traumatic brain injury in vivo
ZJ43
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i.e. (S)-2-[3-((S)-1-carboxy-3-methylbutyl)ureido]pentanedioic acid
[HO2C(CH2)2CH(CO2H)CH2]2P(O)(OH)
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-
additional information
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