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ABSTRACT:
SUBMITTER: Barinka C
PROVIDER: S-EPMC5516903 | biostudies-literature | 2008 Dec
REPOSITORIES: biostudies-literature
Barinka Cyril C Byun Youngjoo Y Dusich Crystal L CL Banerjee Sangeeta R SR Chen Ying Y Castanares Mark M Kozikowski Alan P AP Mease Ronnie C RC Pomper Martin G MG Lubkowski Jacek J
Journal of medicinal chemistry 20081201 24
Urea-based, low molecular weight ligands of glutamate carboxypeptidase II (GCPII) have demonstrated efficacy in various models of neurological disorders and can serve as imaging agents for prostate cancer. To enhance further development of such compounds, we determined X-ray structures of four complexes between human GCPII and urea-based inhibitors at high resolution. All ligands demonstrate an invariant glutarate moiety within the S1' pocket of the enzyme. The ureido linkage between P1 and P1' ...[more]