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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

The Microcystins and Nodularins: Cyclic Polypeptide Inhibitors of PP1 and PP2A

Author(s): B. M. Gulledge, J. B. Aggen, H.- B. Huang, A. C. Nairn and A. R. Chamberlin

Volume 9 , Issue 22 , 2002

Page: [1991 - 2003] Pages: 13

DOI: 10.2174/0929867023368845

Price: $65

Abstract

The serine / threonine phosphatases are inhibited by a variety of natural toxins, including the microcystins and nodularins. Progress in understanding the details of the biosynthetic origin and the binding of these compounds is discussed, as is the progress made in synthesizing the members of these families. Additionally, the work by several groups to either synthesize simplified analogues that are still potent, or introduce selectivity for PP1 over PP2A are discussed. Finally, the properties of a series of five new truncated analogues are examined.

Keywords: Microcystins, PP1, PP2A, threonine phosphatases


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