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Synthesis and biological activity of a focused library of mitogen-activated protein kinase phosphatase inhibitors

Arnold, DM and Foster, C and Huryn, DM and Lazo, JS and Johnston, PA and Wipf, P (2007) Synthesis and biological activity of a focused library of mitogen-activated protein kinase phosphatase inhibitors. Chemical Biology and Drug Design, 69 (1). 23 - 30. ISSN 1747-0277

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Mitogen-activated protein kinase phosphatase 1 is a tyrosine phosphatase superfamily member that dephosphorylates and inactivates mitogen-activated protein kinase substrates, such as p38, c-Jun-N-terminal kinase, and extracellular signal-related kinase. These mitogen-activated protein kinase substrates regulate many cellular processes associated with human diseases. In spite of this potential as a molecular target for chemotherapy, however, pharmacologically tractable inhibitors of mitogen-activated protein kinase phosphatase-1 have yet to be developed. Based on the results from a high-throughput screen for small molecule inhibitors of mitogen-activated protein kinase phosphatase-1, we designed, synthesized, and evaluated a focused library in an effort to further understand the structural requirements for mitogen-activated protein kinase phosphatase-1 inhibitory activity. © 2007 The Authors.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Arnold, DM
Foster, C
Huryn, DM
Lazo, JS
Johnston, PApaj18@pitt.eduPAJ180000-0001-5815-3091
Wipf, Ppwipf@pitt.eduPWIPF
Date: 1 January 2007
Date Type: Publication
Journal or Publication Title: Chemical Biology and Drug Design
Volume: 69
Number: 1
Page Range: 23 - 30
DOI or Unique Handle: 10.1111/j.1747-0285.2007.00474.x
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 1747-0277
MeSH Headings: Cell Cycle Proteins--antagonists & inhibitors; Cell Cycle Proteins--metabolism; Dual Specificity Phosphatase 1; Enzyme Activation; Extracellular Signal-Regulated MAP Kinases--antagonists & inhibitors; Extracellular Signal-Regulated MAP Kinases--metabolism; Humans; Immediate-Early Proteins--antagonists & inhibitors; Immediate-Early Proteins--metabolism; JNK Mitogen-Activated Protein Kinases--antagonists & inhibitors; JNK Mitogen-Activated Protein Kinases--metabolism; Peptide Library; Phosphoprotein Phosphatases--antagonists & inhibitors; Phosphoprotein Phosphatases--metabolism; Phosphorylation; Protein Kinase Inhibitors--chemical synthesis; Protein Kinase Inhibitors--metabolism; Protein Kinase Inhibitors--pharmacology; Protein Phosphatase 1; Protein Tyrosine Phosphatases--antagonists & inhibitors; Protein Tyrosine Phosphatases--metabolism; p38 Mitogen-Activated Protein Kinases--antagonists & inhibitors; p38 Mitogen-Activated Protein Kinases--metabolism
PubMed ID: 17313454
Date Deposited: 07 Jul 2014 16:21
Last Modified: 12 Sep 2019 19:55


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