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

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

Affiliation:

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.

Cite this article as:

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