2or4

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{{STRUCTURE_2or4| PDB=2or4 | SCENE= }}
{{STRUCTURE_2or4| PDB=2or4 | SCENE= }}
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'''A high resolution crystal structure of human glutamate carboxypeptidase II in complex with quisqualic acid'''
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===A high resolution crystal structure of human glutamate carboxypeptidase II in complex with quisqualic acid===
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==Overview==
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Inhibition of glutamate carboxypeptidase II (GCPII) has been shown to be neuroprotective in multiple preclinical models in which dysregulated glutamatergic transmission is implicated. Herein, we report crystal structures of the human GCPII complexed with three glutamate mimetics/derivatives, 2-(phosphonomethyl)pentanedioic acid (2-PMPA), quisqualic acid (QA), and L-serine O-sulfate (L-SOS), at 1.72, 1.62, and 2.10 A resolution, respectively. Despite the structural differences between the distal parts of the inhibitors, all three compounds share similar binding modes in the pharmacophore (i.e., S1') pocket of GCPII, where they are stabilized by a combination of polar and van der Waals interactions. The structural diversity of the distal parts of the inhibitors leads to rearrangements of the S1' site that are necessary for efficient interactions between the enzyme and an inhibitor. The set of structures presented here, in conjunction with the available biochemical data, illustrates a flexibility of the GCPII pharmacophore pocket and highlights the structural features required for potent GCPII inhibition. These findings could facilitate the rational structure-based drug design of new GCPII inhibitors in the future.
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(as it appears on PubMed at http://www.pubmed.gov), where 17567119 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17567119}}
==About this Structure==
==About this Structure==
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[[Category: Naaladase]]
[[Category: Naaladase]]
[[Category: Prostate specific membrane antigen]]
[[Category: Prostate specific membrane antigen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:30:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 13:28:19 2008''

Revision as of 10:28, 28 July 2008

Image:2or4.png

Template:STRUCTURE 2or4

A high resolution crystal structure of human glutamate carboxypeptidase II in complex with quisqualic acid

Template:ABSTRACT PUBMED 17567119

About this Structure

2OR4 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II., Barinka C, Rovenska M, Mlcochova P, Hlouchova K, Plechanovova A, Majer P, Tsukamoto T, Slusher BS, Konvalinka J, Lubkowski J, J Med Chem. 2007 Jul 12;50(14):3267-73. Epub 2007 Jun 14. PMID:17567119

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