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Literature summary for 3.4.17.21 extracted from

  • Thomas, A.G.; Wozniak, K.M.; Tsukamoto, T.; Calvin, D.; Wu, Y.; Rojas, C.; Vornov, J.; Slusher, B.S.
    Glutamate carboxypeptidase II (NAALADase) inhibition as a novel therapeutic strategy (2006), Adv. Exp. Med. Biol., 576, 327-37.
    View publication on PubMed
Search for more literature for 3.4.17.21

Application

Application Comment Organism
pharmacology the enzyme is a target for specific inhibitor design in therapy of neurodegenerative disorders, overview Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
2-(3-mercaptopropyl)-pentanedioic acid 2-MPPA, specific, potent, competitive inhibition, has higher oral bioavailability compared to 2-PMPA, acts neuroprotective in vivo, e.g. in case of ischemic stroke, and provides analgesia Homo sapiens
2-(3-mercaptopropyl)-pentanedioic acid 2-MPPA, specific, potent, competitive inhibition, acts neuroprotective in vivo, e.g. in case of ischemic stroke, and provides analgesia Rattus norvegicus
2-(phosphonomethyl)-pentanedioic acid 2-PMPA, specific, potent, competitive inhibition, acts neuroprotective in vivo, e.g. in case of ischemic stroke, and provides analgesia Homo sapiens
2-(phosphonomethyl)-pentanedioic acid 2-PMPA, specific, potent, competitive inhibition, acts neuroprotective in vivo, e.g. in case of ischemic stroke, and provides analgesia Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
brush border
-
 Homo sapiens 5903
-
membrane
-
 Homo sapiens 16020
-
plasma membrane
-
 Homo sapiens 5886
-

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ interacts with the glutamate recognition site Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O Homo sapiens the enzyme is involved in glutamate-mediated neurodegenerative disorders, enzyme inhibition is a mechanism for reduction of excitotoxic glutamate N-acetyl-alpha-L-aspartate + L-glutamate
-
 ?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O Rattus norvegicus the enzyme is involved in glutamate-mediated neurodegenerative disorders, enzyme inhibition is a mechanism for reduction of excitotoxic glutamate N-acetyl-alpha-L-aspartate + L-glutamate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 bifunctional enzyme
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
 Homo sapiens
-
brain
-
 Rattus norvegicus
-
glial cell
-
 Homo sapiens
-
prostate cancer cell
-
 Homo sapiens
-
prostate gland prostate form of the enzyme is termed prostate-specific membrane antigen Homo sapiens
-
small intestine membrane brush border Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information bifunctional enzyme performing folate hydrolase and N-acetylated alpha-linked acidic dipeptidase, NAALADase, activities Homo sapiens ?
-
 ?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O the enzyme is involved in glutamate-mediated neurodegenerative disorders, enzyme inhibition is a mechanism for reduction of excitotoxic glutamate Homo sapiens N-acetyl-alpha-L-aspartate + L-glutamate
-
 ?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O the enzyme is involved in glutamate-mediated neurodegenerative disorders, enzyme inhibition is a mechanism for reduction of excitotoxic glutamate Rattus norvegicus N-acetyl-alpha-L-aspartate + L-glutamate
-
 ?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O i.e. NAAG Homo sapiens N-acetyl-alpha-L-aspartate + L-glutamate
-
 ?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O i.e. NAAG Rattus norvegicus N-acetyl-alpha-L-aspartate + L-glutamate
-
 ?

Synonyms

Synonyms Comment Organism
GCP II
-
 Homo sapiens
GCP II
-
 Rattus norvegicus
N-Acetylated alpha-linked acidic dipeptidase
-
 Homo sapiens
N-Acetylated alpha-linked acidic dipeptidase
-
 Rattus norvegicus
NAALADase
-
 Homo sapiens
NAALADase
-
 Rattus norvegicus
Prostate-specific membrane antigen
-
 Homo sapiens
PSMA
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000002
-
 2-(phosphonomethyl)-pentanedioic acid
-
 Homo sapiens
0.00003
-
 2-(3-mercaptopropyl)-pentanedioic acid
-
 Homo sapiens