| Literature DB >> 17336521 |
Patrick T Gunning1, William P Katt, Matthew Glenn, Khandaker Siddiquee, Khandaker Siddique, Joon S Kim, Richard Jove, Saïd M Sebti, James Turkson, Andrew D Hamilton.
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 (IC(50) value of 31 microM) relative to STAT3 (IC(50) value of 560 microM).Entities:
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Year: 2007 PMID： 17336521 DOI： 10.1016/j.bmcl.2007.01.077
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823