Protein Phosphatase Inhibition: Structure Based Design. Towards New Therapeutic Agents

Authors: Sakoff, Jennette A.; McCluskey, Adam

Source: Current Pharmaceutical Design, Volume 10, Number 10, April 2004 , pp. 1139-1159(21)

Publisher: Bentham Science Publishers

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Abstract:

Cellular signalling processes are governed by a delicate balance of phosphatase and kinase activity. Over the past few years there has been considerable effort directed toward the development of kinase based therapeutic agents, whilst phosphatase based therapeutics have lagged. Herein we address key issues relating to selected therapeutic targets: malignancy, diabetes, immunosuppression, cystic fibrosis, asthma and cardiovascular disease. As part of ongoing studies we examine the recent developments in understanding the key interactions between the okadaic acid class of compounds and the serine / threonine protein phosphatases 1, 2A and 2B. Crystal structure and molecular modelling guided inhibitor development is also a key focus of this article.

Keywords: protein phosphatase inhibition; structure based design; okadaic acid; serine/threonine protein phosphatases

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612043452686

Affiliations: 1: Chemistry, School of Environmental and Life Sciences, The University of Newcastle, University Drive, Callaghan, NSW, Australia 2308.

Publication date: 2004-04-01

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Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.

Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.