Generic placeholder image

Current Medicinal Chemistry

Editor-in-Chief

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

Okadaic Acid: The Archetypal Serine / Threonine Protein Phosphatase Inhibitor

Author(s): A. B. Dounay and C. J. Forsyth

Volume 9 , Issue 22 , 2002

Page: [1939 - 1980] Pages: 42

DOI: 10.2174/0929867023368791

Price: $65

Abstract

As the first recognized member of the “okadaic acid class” of phosphatase inhibitors, the marine natural product okadaic acid is perhaps the most well-known member of a diverse array of secondary metabolites that have emerged as valuable probes for studying the roles of various cellular protein serine / threonine phosphatases. This review provides a historical perspective on the role that okadaic acid has played in stimulating a broad spectrum of modern scientific research as a result of the natural products ability to bind to and inhibit important classes of protein serine / threonine phosphatases. The relationships between the structure and biological activities of okadaic acid are briefly reviewed, as well as the structural information regarding the particular cellular receptors protein phosphatases 1 (PP1) and 2A. Laboratory syntheses of okadaic acid and its analogs are thoroughly reviewed. Finally, an interpretation of the critical contacts observed between okadaic acid and PP1 by X-ray crystallography is provided, and specific molecular recognition hypotheses that are testable via the synthesis and assay of non-natural analogs of okadaic acid are suggested.

Keywords: Okadaic Acid, threonine phosphatases, crystallography


Rights & Permissions Print Export Cite as
© 2022 Bentham Science Publishers | Privacy Policy