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Literature summary for 3.4.17.21 extracted from

  • Hlouchova, K.; Barinka, C.; Konvalinka, J.; Lubkowski, J.
    Structural insight into the evolutionary and pharmacologic homology of glutamate carboxypeptidases II and III (2009), FEBS J., 276, 4448-4462.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
GCPIII ectodomain in a pseudo-unliganded state and in a complex with product L-glutamate, or the phosphapeptide transition state mimetic (2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid, or quisqualic acid, a glutamate biostere, X-ray diffraction structure determination and analysis at 1.29-1.56 A resolution, modelling Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid EPE, a phosphapeptide transition state analog of glutamyl-glutamate Homo sapiens
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 Homo sapiens
L-Glu
-
Homo sapiens
MOPS
-
Homo sapiens
additional information GCPIII enzyme-inhibitor interactions and the architecture of the S1' pocket, overview Homo sapiens

Localization

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

Metals/Ions

Metals/Ions Comment Organism Structure
additional information GCPIII and GCPII are metalloenzymes Homo sapiens
Zn2+ binding structure of Zn2+ ions in the bimetallic active site, overview 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
-
L-glutamate + N-acetyl-L-aspartate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
nervous system GCPII Homo sapiens
-
prostate GCPII Homo sapiens
-
small intestine GCPII Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the S1' pocket, the pharmacophore pocket of GCPIII, is shaped by residues Phe199, Arg200, Asn247, Glu414, Gly417, Leu418, Gly508, Tyr542, Lys689 and Tyr690. The specificity of GCPIII towards the P1' glutamate (or glutamate-like moieties) is determined by a combination of ionic and polar interactionsGCPIII substrate-binding cavity structure, overview Homo sapiens ?
-
?
N-acetyl-L-aspartyl-L-glutamate + H2O
-
Homo sapiens L-glutamate + N-acetyl-L-aspartate
-
?

Subunits

Subunits Comment Organism
More overall fold and quaternary arrangement of the GCPIII molecule, overview Homo sapiens

Synonyms

Synonyms Comment Organism
GCPII
-
Homo sapiens
GCPIII
-
Homo sapiens
glutamate carboxypeptidase II
-
Homo sapiens
glutamate carboxypeptidase III
-
Homo sapiens
More glutamate carboxypeptidase III and glutamate carboxypeptidase II belong to the transferrin receptor/glutamate carboxypeptidase II superfamily Homo sapiens
NAALADase
-
Homo sapiens
prostate specific membrane antigen
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000129
-
(2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid GCPII Homo sapiens
0.0000346
-
(2S,3'S)-[[(3'-amino-3'-carboxy-propyl)-hydroxyphosphinoyl]methyl]-pentanedioic acid GCPIII Homo sapiens
0.00023
-
2-amino-3-(3,5-dioxo[1,2,4]oxadiazolidin-2-yl)propionic acid GCPIII Homo sapiens
0.00102
-
2-amino-3-(3,5-dioxo[1,2,4]oxadiazolidin-2-yl)propionic acid GCPII Homo sapiens
0.27
-
L-Glu GCPIII Homo sapiens
0.428
-
L-Glu GCPII Homo sapiens