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Literature summary for 3.4.17.21 extracted from

  • Novakova, Z.; Wozniak, K.; Jancarik, A.; Rais, R.; Wu, Y.; Pavlicek, J.; Ferraris, D.; Havlinova, B.; Ptacek, J.; Vavra, J.; Hin, N.; Rojas, C.; Majer, P.; Slusher, B.S.; Tsukamoto, T.; Barinka, C.
    Unprecedented binding mode of hydroxamate-based inhibitors of glutamate carboxypeptidase II structural characterization and biological activity (2016), J. Med. Chem., 59, 4539-4550 .
    View publication on PubMed

Application

Application Comment Organism
medicine glutamate carboxypeptidase II is effective in preclinical models of neurological disorders associated with excessive activation of glutamatergic systems. The study validates the use of hydroxamate-based inhibitors in the treatment of a chronic neurological disorder such as neuropathic pain Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
X-ray structure of human glutamate carboxypeptidase II in complex with hydroxamate-based inhibitors Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-[(2-(R))-2-carboxy-5-(oxidanylamino)-5-oxidanylidene-pentyl]benzoic acid
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Homo sapiens
4-[(2-(S))-2-carboxy-5-(oxidanylamino)-5-oxidanylidene-pentyl]benzoic acid
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Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04609
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-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information enzyme/hydroxamate complexes reveal an unprecedented binding mode in which the putative P1' glutarate occupies the spacious entrance funnel rather than the conserved glutamate-binding S1' pocket. This unique binding mode provides a mechanistic explanation for the structure-activity relationship data, most notably the lack of enantiospecificity and the tolerance for bulky/hydrophobic functions as substituents of a canonical glutarate moiety Homo sapiens ?
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Synonyms

Synonyms Comment Organism
GCPII
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Homo sapiens
glutamate carboxypeptidase II
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Homo sapiens