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Cindy J. Choy, Melody D. Fulton, Austen L. Davis, Mark Hopkins, Joseph K. Choi, Marc O. Anderson and Clifford E. Berkman Rationally Designed Sulfamides as Glutamate Carboxypeptidase II Inhibitors Chemical Biology & Drug Design 82

Article first published online: 25 SEP 2013 | DOI: 10.1111/cbdd.12174

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This current study explores a new class of GCPII inhibitors, glutamyl sulfamides, which possess a neutral tetrahedral zinc-binding motif. A small library containing six sulfamides was prepared and evaluated for inhibitory potency against purified GCPII. While most inhibitors have potencies in the micromolar range, one showed promising sub-micromolar potency, with the optimal inhibitor in this series being aspartyl-glutamyl sulfamide.

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