Yale University;University of South Florida;University of Central Florida Research Foundation, Inc.
发明人:
TURKSON, JAMES,HAMILTON, ANDREW D.,JOVE, RICHARD,SEBTI, SAID M.
申请号：
PL07868993
公开号：
PL2120958T3
申请日:
2007.12.05
申请国别(地区):
PL
年份:
2013
代理人:
摘要：
A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.
