发明名称 |
Stat3 inhibitor having anti-cancer activity and methods |
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. |
申请公布号 |
US8609639(B2) |
申请公布日期 |
2013.12.17 |
申请号 |
US20070517453 |
申请日期 |
2007.12.05 |
申请人 |
TURKSON JAMES;SEBTI SAID;JOVE RICHARD;HAMILTON ANDREW D.;UNIVERSITY OF SOUTH FLORIDA;YALE UNIVERSITY;UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC. |
发明人 |
TURKSON JAMES;SEBTI SAID;JOVE RICHARD;HAMILTON ANDREW D. |
分类号 |
A61K31/675;C07F9/653;C12N5/071 |
主分类号 |
A61K31/675 |
代理机构 |
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代理人 |
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