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

David   A.   Colby; A.   R.   Chamberlin

doi:10.2174/138955706777435715

Abstract

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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Mini-Reviews in Medicinal Chemistry

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

Volume: 6 Issue: 6

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

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

Abstract: 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.

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Colby A. David and Chamberlin R. A., Pharmacophore Identification: The Case of the Ser/Thr Protein Phosphatase Inhibitors, Mini-Reviews in Medicinal Chemistry 2006; 6 (6) . https://dx.doi.org/10.2174/138955706777435715