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Small molecule inhibitors of dual specificity protein phosphatases

Pestell, KE and Ducruet, AP and Wipf, P and Lazo, JS (2000) Small molecule inhibitors of dual specificity protein phosphatases. Oncogene, 19 (56). 6607 - 6612. ISSN 0950-9232

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One hallmark of neoplasia is the deregulation of cell cycle control mechanisms, which is secondary to altered protein phosphorylation. Dual specificity protein phosphatases uniquely dephosphorylate both phosphoserines/threonines and phosphotyrosines on the same protein substrate. As a class they regulate intracellular signaling through the mitogen activated and stress activated kinases and govern cellular movement through G1/S and G2/M cell cycle checkpoints by affecting the activity of cyclin-dependent kinases. In particular, the Cdc25 phosphatases, which dephosphorylate cyclin-dependent kinases, are overexpressed in many human tumors and this increased expression is associated with a poor prognosis. In addition to expression levels, the intracellular activity of Cdc25 phosphatases is determined by their subcellular distribution and physical proximity to substrates. Small molecules that either inhibit the catalytic activity or alter the subcellular distribution of these dual specificity protein phosphatases could provide effective tools to interrogate the role of phosphorylation pathways and may afford new approaches to the management of cancer.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Pestell, KE
Ducruet, AP
Wipf, Ppwipf@pitt.eduPWIPF
Lazo, JS
Date: 27 December 2000
Date Type: Publication
Journal or Publication Title: Oncogene
Volume: 19
Number: 56
Page Range: 6607 - 6612
DOI or Unique Handle: 10.1038/sj.onc.1204084
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 0950-9232
Article Type: Review
MeSH Headings: Animals; Antineoplastic Agents--pharmacology; Cyclin-Dependent Kinases--metabolism; Enzyme Inhibitors--pharmacology; Humans; Models, Biological; Neoplasms--metabolism; Protein Tyrosine Phosphatases--antagonists & inhibitors; Protein Tyrosine Phosphatases--chemistry; Protein Tyrosine Phosphatases--metabolism; cdc25 Phosphatases--antagonists & inhibitors; cdc25 Phosphatases--chemistry; cdc25 Phosphatases--metabolism
PubMed ID: 11426646
Date Deposited: 17 Feb 2014 20:02
Last Modified: 02 Feb 2019 15:57


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