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Literature summary for 3.4.17.21 extracted from

  • Knedlik, T.; Vorlova, B.; Navratil, V.; Tykvart, J.; Sedlak, F.; Vaculin, S.; Franek, M.; Sacha, P.; Konvalinka, J.
    Mouse glutamate carboxypeptidase II (GCPII) has a similar enzyme activity and inhibition profile but a different tissue distribution to human GCPII (2017), FEBS Open Bio, 7, 1362-1378 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.17.21

Application

Application Comment Organism
diagnostics the enzyme is an important diagnostic marker of prostate cancer progression Homo sapiens
medicine the enzyme is a putative target for the treatment of both prostate cancer and neuronal disorders associated with glutamate excitotoxicity Homo sapiens
medicine the enzyme is an important diagnostic marker of prostate cancer progression and a putative target for the treatment of both prostate cancer and neuronal disorders associated with glutamate excitotoxicity. For the development of novel therapeutics, mouse models are used. Differences in enzymatic activity and inhibition profile are small. Therefore, mouse glutamate carboxypeptidase II can approximate human glutamate carboxypeptidase II in drug development and testing. On the other hand, significant differences in glutamate carboxypeptidase II tissue expression must be taken into account when developing novel glutamate carboxypeptidase II-based anticancer and therapeutic methods, including targeted anticancer drug delivery systems, and when using mice as a model organism Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens
-
 Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid
-
 Homo sapiens
(2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid
-
 Mus musculus
2-(phosphonomethyl)pentanedioic acid
-
 Homo sapiens
2-(phosphonomethyl)pentanedioic acid
-
 Mus musculus
N-[4-carboxy-3-(carboxymethyl)-3-hydroxybutanoyl]-L-glutamic acid
-
 Homo sapiens
N-[4-carboxy-3-(carboxymethyl)-3-hydroxybutanoyl]-L-glutamic acid
-
 Mus musculus
N-[[(1S)-1-carboxy-3-methylbutyl]carbamoyl]-L-glutamic acid
-
 Homo sapiens
N-[[(1S)-1-carboxy-3-methylbutyl]carbamoyl]-L-glutamic acid
-
 Mus musculus
N-[[(1S)-1-carboxy-5-(4-iodobenzamido)pentyl]carbamoyl]-L-glutamic acid
-
 Homo sapiens
N-[[(1S)-1-carboxy-5-(4-iodobenzamido)pentyl]carbamoyl]-L-glutamic acid
-
 Mus musculus
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
-
 Homo sapiens
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
-
 Mus musculus
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
-
 Homo sapiens
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
-
 Mus musculus
N-[[(1S)-5-acetamido-1-carboxypentyl]carbamoyl]-L-glutamic acid
-
 Homo sapiens
N-[[(1S)-5-acetamido-1-carboxypentyl]carbamoyl]-L-glutamic acid
-
 Mus musculus
N-[[(1S)-5-[acetyl[(4-bromophenyl)methyl]amino]-1-carboxypentyl]carbamoyl]-L-glutamic acid
-
 Homo sapiens
N-[[(1S)-5-[acetyl[(4-bromophenyl)methyl]amino]-1-carboxypentyl]carbamoyl]-L-glutamic acid
-
 Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000039
-
 pteroyl-di-L-glutamate pH 7.4, 37°C Homo sapiens
0.00029
-
 pteroyl-di-L-glutamate pH 7.4, 37°C Mus musculus
0.00055
-
 N-acetyl-L-aspartyl-L-glutamate pH 7.4, 37°C Homo sapiens
0.0019
-
 N-acetyl-L-aspartyl-L-glutamate pH 7.4, 37°C Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04609
-
-
Mus musculus O35409
-
-

Purification (Commentary)

Purification (Comment) Organism
efficient one-step purification method yields purified recombinant enzyme Homo sapiens
efficient one-step purification method yields purified recombinant enzyme Mus musculus

Source Tissue

Source Tissue Comment Organism Textmining
brain high expression Mus musculus
-
brain considerably increased in prostate carcinoma Homo sapiens
-
kidney high expression Mus musculus
-
additional information no activity detected in mouse prostate Mus musculus
-
prostate gland
-
 Homo sapiens
-
prostate gland cancer cell considerably increased in prostate carcinoma Homo sapiens
-
salivary gland high expression Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information mouse glutamate carboxypeptidase II possesses lower catalytic efficiency but similar substrate specificity compared with the human protein Mus musculus ?
-
 ?
N-acetyl-L-aspartyl-L-glutamate + H2O
-
 Homo sapiens N-acetyl-L-aspartate + L-glutamate
-
 ?
N-acetyl-L-aspartyl-L-glutamate + H2O
-
 Mus musculus N-acetyl-L-aspartate + L-glutamate
-
 ?
pteroyl-di-L-glutamate + H2O
-
 Homo sapiens L-Glu + pteroylglutamate
-
 ?
pteroyl-di-L-glutamate + H2O
-
 Mus musculus L-Glu + pteroylglutamate
-
 ?

Synonyms

Synonyms Comment Organism
folate hydrolase
-
 Homo sapiens
folate hydrolase
-
 Mus musculus
GCPII
-
 Homo sapiens
GCPII
-
 Mus musculus
glutamate carboxypeptidase II
-
 Homo sapiens
glutamate carboxypeptidase II
-
 Mus musculus
Prostate-specific membrane antigen
-
 Homo sapiens
Prostate-specific membrane antigen
-
 Mus musculus
PSMA
-
 Homo sapiens
PSMA
-
 Mus musculus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.44
-
 N-acetyl-L-aspartyl-L-glutamate pH 7.4, 37°C Mus musculus
1.45
-
 N-acetyl-L-aspartyl-L-glutamate pH 7.4, 37°C Homo sapiens
3.63
-
 pteroyl-di-L-glutamate pH 7.4, 37°C Mus musculus
5.09
-
 pteroyl-di-L-glutamate pH 7.4, 37°C Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000017
-
 N-[[(1S)-1-carboxy-5-(4-iodobenzamido)pentyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Homo sapiens
0.000000018
-
 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 37°C, pH 7.4 Homo sapiens
0.000000021
-
 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 37°C, pH 7.4 Homo sapiens
0.000000028
-
 N-[[(1S)-1-carboxy-5-(4-iodobenzamido)pentyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Mus musculus
0.000000049
-
 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 37°C, pH 7.4 Mus musculus
0.00000005
-
 N-[[(1S)-5-[acetyl[(4-bromophenyl)methyl]amino]-1-carboxypentyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Homo sapiens
0.0000001
-
 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 37°C, pH 7.4 Mus musculus
0.00000017
-
 N-[[(1S)-5-acetamido-1-carboxypentyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Homo sapiens
0.00000026
-
 2-(phosphonomethyl)pentanedioic acid 37°C, pH 7.4 Homo sapiens
0.00000056
-
 2-(phosphonomethyl)pentanedioic acid 37°C, pH 7.4 Mus musculus
0.00000058
-
 N-[[(1S)-1-carboxy-3-methylbutyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Homo sapiens
0.00000066
-
 N-[[(1S)-5-acetamido-1-carboxypentyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Mus musculus
0.00000068
-
 N-[[(1S)-5-[acetyl[(4-bromophenyl)methyl]amino]-1-carboxypentyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Mus musculus
0.0000059
-
 N-[[(1S)-1-carboxy-3-methylbutyl]carbamoyl]-L-glutamic acid 37°C, pH 7.4 Mus musculus
0.00052
-
 (2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid 37°C, pH 7.4 Homo sapiens
0.00058
-
 (2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid 37°C, pH 7.4 Mus musculus
0.016
-
 N-[4-carboxy-3-(carboxymethyl)-3-hydroxybutanoyl]-L-glutamic acid 37°C, pH 7.4 Homo sapiens
0.024
-
 N-[4-carboxy-3-(carboxymethyl)-3-hydroxybutanoyl]-L-glutamic acid 37°C, pH 7.4 Mus musculus

General Information

General Information Comment Organism
physiological function the enzyme participates in glutamate excitotoxicity in the brain Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
757
-
 N-acetyl-L-aspartyl-L-glutamate pH 7.4, 37°C Mus musculus
2900
-
 N-acetyl-L-aspartyl-L-glutamate pH 7.4, 37°C Homo sapiens
12517
-
 pteroyl-di-L-glutamate pH 7.4, 37°C Mus musculus
130513
-
 pteroyl-di-L-glutamate pH 7.4, 37°C Homo sapiens