Document Type
Patent
Publication Date
December 2013
Patent Number
8609639
Abstract
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.
Application Number
12/517,453
Recommended Citation
Turkson, James; Sebti, Said; Jove, Richard; and Hamilton, Andrew D., "Stat3 inhibitor having anti-cancer activity and methods" (2013). USF Patents. 282.
https://digitalcommons.usf.edu/usf_patents/282
Assignees
University of South Florida Yale University University of Central Florida Research Foundation, Inc.
Filing Date
12/05/2007
Primary/U.S. Class
514/92
