2jbj | pdb_00002jbj

MEMBRANE-BOUND GLUTAMATE CARBOXYPEPTIDASE II (GCPII) IN COMPLEX WITH 2-PMPA (2-PHOSPHONOMETHYL-PENTANEDIOIC ACID)

File:2jbj.gif

spinqualitylabelsall models 2jbj, resolution 2.19Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D

Overview

Human glutamate carboxypeptidase II (GCPII) occurs in the central nervous, system as well as in human prostate (where it is called prostate-specific, membrane antigen; PSMA). Inhibitors of the enzyme have been shown to, provide neuroprotection, but may also be useful for the detection, imaging, and treatment of prostate cancer. Crystal structures were determined of, the extracellular part of GCPII (amino-acid residues 44-750) in complex, with two potent inhibitors, quisqualate and 2-PMPA (the strongest GCPII, inhibitor to date), at resolutions of 3.0 and 2.2 A, respectively. In, addition, models were constructed for binding of the inhibitors, willardiine, homoibotenate, L-2-amino-4-phosphonobutanoic acid and, L-serine-O-sulfate to the S1' site of the enzyme. The common denominator, for high-affinity binding to the S1' site is the formation of two strong, salt bridges.

Disease

Known diseases associated with this structure: Myocardial infarcation, susceptibility to OMIM:[602855]

About this Structure

2JBJ is a Single protein structure of sequence from Homo sapiens with NAG, ZN, CA, CL and G88 as ligands. Active as Glutamate carboxypeptidase II, with EC number 3.4.17.21 Known structural/functional Sites: AC1, AC2, AC3, AC4, AC5, AC6, AC7, AC8, BC1, BC2, BC3, BC4, BC5, BC6, BC7, BC8 and BC9. Full crystallographic information is available from OCA.

Reference

Human glutamate carboxypeptidase II inhibition: structures of GCPII in complex with two potent inhibitors, quisqualate and 2-PMPA., Mesters JR, Henning K, Hilgenfeld R, Acta Crystallogr D Biol Crystallogr. 2007 Apr;63(Pt 4):508-13. Epub 2007, Mar 16. PMID:17372356

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