Authors: Hoffman, Brian T.; Nelson, Melanie R.; Burdick, Keith; Baxter, Susan M.

Source: Current Pharmaceutical Design, Volume 10, Number 10, April 2004 , pp. 1161-1181(21)

Publisher: Bentham Science Publishers

Abstract:

The Protein Tyrosine Phosphatase (PTP) family contains not only several promising drug targets, such as PTP1B, but also proteins that are essential to cell development and survival. The availability of sequences and representative structures for the PTP family allows better identification of anti-targets, closely related family members likely to cross-react with directed inhibitors. Eight PTP subfamilies, classified by active site information and overall PTP catalytic domain structure similarity, are reviewed here: 1) the tyrosine-specific PTPs, 2) the dualspecificity PTPs, 3) the cdc25 subclass; 4) the Pten subclass; 5) the myotubularins, 6) the PRL subclass, 7) the low molecular weight PTPs, and 8) the newly defined cdc14 subclass. PTP subfamily classification and structure information can be incorporated into design strategies aimed at identifying potent and selective small molecule inhibitors. The accumulating inhibition data for compounds screened against panels of PTPs is reviewed. The in vitro data can yield clues to specificity so that individual subfamilies can be matched with effective scaffolds to jumpstart lead design and reduce false starts.

Keywords: protein tyrosine phosphatases; ptp; dual-specificity phosphatases; structure-based drug design; inhibitor; specificity

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612043452659

Affiliations: 1: Cengent Therapeutics, 10929 Technology Place, San Diego, CA 92127.

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.

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