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
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
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.
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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
DOI https://dx.doi.org/10.2174/138955706777435715 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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