Title
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: Structural recognition of STAT SH2 domains
Abbreviated Journal Title
Bioorg. Med. Chem. Lett.
Keywords
STAT1; STAT3; peptidomimetics; inhibitors; anti-cancer; SH2 domain; recognition; SIGNAL TRANSDUCER; MOLECULAR TARGETS; GENE-REGULATION; ACTIVATOR; DNA; PATHWAY; Chemistry, Medicinal; Chemistry, Organic
Abstract
The identification of constitutively activated STAT (Signal Transducers and Activators of Transcription) proteins in aberrant cell signaling pathways has led to investigations targeting the selective disruption of specific STAT isoforms directly associated with oncogenisis. We have identified, through the design of a library of peptidomimetic inhibitors, agents that selectively disrupt STAT1 or STAT3 homo-dimerization at low micromolar concentrations. ISS840 has 20-fold higher inhibition of STAT1 homo-dimerization (IC50 value of 31 mu M) relative to STAT3 (IC50 value of 560 mu M). (c) 2007 Published by Elsevier Ltd.
Journal Title
Bioorganic & Medicinal Chemistry Letters
Volume
17
Issue/Number
7
Publication Date
1-1-2007
Document Type
Article
Language
English
First Page
1875
Last Page
1878
WOS Identifier
ISSN
0960-894X
Recommended Citation
"Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: Structural recognition of STAT SH2 domains" (2007). Faculty Bibliography 2000s. 7186.
https://stars.library.ucf.edu/facultybib2000/7186
Comments
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