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

[ Vol. 6 , Issue. 6 ]


David A. Colby and A. R. Chamberlin   Pages 657 - 665 ( 9 )


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.


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


Department of Chemistry,University of California at Irvine, Irvine, CA 92697, USA.

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