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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Pharmacophore Identification: The Case of the Ser/Thr Protein Phosphatase Inhibitors

Author(s): David A. Colby and A. R. Chamberlin

Volume 6, Issue 6, 2006

Page: [657 - 665] Pages: 9

DOI: 10.2174/138955706777435715

Price: $65


This review provides a chronological account of the identification and refinement of the pharmacophore for inhibition of two key serine/threonine protein phosphatases, PP1 and PP2A. The dramatic impact of natural product isolation, molecular modeling, analogue design, biochemical studies, and crystallography on the evolution of the pharmacophore will be described.

Keywords: Protein phosphatase, PP1, PP2A, okadaic acid, microcystin, tautomycin, fostriecin, calyculin

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