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.
STAT1; STAT3; peptidomimetics; inhibitors; anti-cancer; SH2 domain; recognition; SIGNAL TRANSDUCER; MOLECULAR TARGETS; GENE-REGULATION; ACTIVATOR; DNA; PATHWAY; Chemistry, Medicinal; Chemistry, Organic
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.
Bioorganic & Medicinal Chemistry Letters
"Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: Structural recognition of STAT SH2 domains" (2007). Faculty Bibliography 2000s. 7186.