Title of article
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: Structural recognition of STAT SH2 domains
Author/Authors
Patrick T. Gunning، نويسنده , , William P. Katt، نويسنده , , Matthew Glenn، نويسنده , , Khandaker Siddique، نويسنده , , Joon S. Kim، نويسنده , , Richard Jove، نويسنده , , Said M. Sebti، نويسنده , , James Turkson، نويسنده , , Andrew D. Hamilton، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
1875
To page
1878
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 μM) relative to STAT3 (IC50 value of 560 μM).
Keywords
STAT3 , peptidomimetics , inhibitors , STAT1 , Anti-cancer , SH2 domain recognition
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797949
Link To Document