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Dual-specificity phosphatases as targets for antineoplastic agents

Lyon, MA and Ducruet, AP and Wipf, P and Lazo, JS (2002) Dual-specificity phosphatases as targets for antineoplastic agents. Nature Reviews Drug Discovery, 1 (12). 961 - 976. ISSN 1474-1776

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Abstract

Dual-specificity protein phosphatases are a subclass of protein tyrosine phosphatases that are uniquely able to hydrolyse the phosphate ester bond on both a tyrosine and a threonine or serine residue on the same protein. Dual-specificity phosphatases have a central role in the complex regulation of signalling pathways that are involved in cell stress responses, proliferation and death. Although this enzyme family is increasingly the target of drug discovery efforts in pharmaceutical companies, a summary of the salient developments in the biology and medicinal chemistry of dual-specificity phosphatases has been lacking. We hope that this comprehensive overview will stimulate further progress in the development of small-molecule inhibitors that could form the basis for a new class of target-directed therapeutic agents.


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Details

Item Type: Article
Status: Published
Creators/Authors:
CreatorsEmailPitt UsernameORCID
Lyon, MA
Ducruet, AP
Wipf, Ppwipf@pitt.eduPWIPF
Lazo, JS
Date: 1 December 2002
Date Type: Publication
Journal or Publication Title: Nature Reviews Drug Discovery
Volume: 1
Number: 12
Page Range: 961 - 976
DOI or Unique Handle: 10.1038/nrd963
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 1474-1776
Article Type: Review
MeSH Headings: Animals; Antineoplastic Agents--pharmacology; Enzyme Inhibitors--pharmacology; Humans; Models, Biological; Neoplasms--metabolism; Protein Tyrosine Phosphatases--antagonists & inhibitors; Protein Tyrosine Phosphatases--chemistry; Protein Tyrosine Phosphatases--metabolism
PubMed ID: 12461518
Date Deposited: 06 Feb 2014 23:36
Last Modified: 02 Feb 2019 15:56
URI: http://d-scholarship.pitt.edu/id/eprint/20446

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