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Literature summary for 3.4.17.21 extracted from

  • Barinka, C.; Byun, Y.; Dusich, C.L.; Banerjee, S.R.; Chen, Y.; Castanares, M.; Kozikowski, A.P.; Mease, R.C.; Pomper, M.G.; Lubkowski, J.
    Interactions between human glutamate carboxypeptidase II and urea-based inhibitors: structural characterization (2008), J. Med. Chem., 51, 7737-7743.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine urea-based, low molecular weight ligands of glutamate carboxypeptidase II have demonstrated efficacy in various models of neurological disorders and can serve as imaging agents for prostate cancer Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
the extracellular part, amino acids 44-750, of human GCPII is cloned and heterologously overexpressed in Drosophila Schneiders S2 cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
the structures of human GCPII in complex with (S)-2-(3-((R)-1-carboxy-(2-methylthio)ethyl)ureido)pentanedioic acid, (S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid, (S)-2-(3-((R)-1-carboxy-2-(4-fluorobenzylthio)ethyl)ureido)pentanedioic acid and (S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid are solved to a resolution of 1.75, 1.54, 1.69 and 1.55 A, respectively Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-2-(3-((R)-1-carboxy-(2-methylthio)ethyl)ureido)pentanedioic acid DCMC Homo sapiens
(S)-2-(3-((R)-1-carboxy-2-(4-fluorobenzylthio)ethyl)ureido)pentanedioic acid DCFBC Homo sapiens
(S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid DCIBzL Homo sapiens
(S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid DCIT Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
N-acetyl-L-aspartyl-L-glutamate + H2O Homo sapiens
-
N-acetyl-L-aspartate + L-glutamate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04609
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
nervous system
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-acetyl-L-aspartyl-L-glutamate + H2O
-
Homo sapiens N-acetyl-L-aspartate + L-glutamate
-
?

Synonyms

Synonyms Comment Organism
GCPII
-
Homo sapiens
glutamate carboxypeptidase II
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000006
-
-
Homo sapiens (S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid
0.0000005
-
-
Homo sapiens (S)-2-(3-((S)-1-carboxy-2-(4-hydroxy-3-iodophenyl)ethyl)ureido)pentanedioic acid
0.000014
-
-
Homo sapiens (S)-2-(3-((R)-1-carboxy-2-(4-fluorobenzylthio)ethyl)ureido)pentanedioic acid
0.000017
-
-
Homo sapiens (S)-2-(3-((R)-1-carboxy-(2-methylthio)ethyl)ureido)pentanedioic acid