Title

STAT3 inhibitor having anti-cancer activity and associated methods (EP)

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.

Document Type

Patent

Patent Number

EP 2 120 958 B1

Application Serial Number

7868993.2

Issue Date

3-20-2013

Current Assignee

Joint Assignment w/UCFRF: Yale University

Assignee at Issuance

Joint Assignment w/UCFRF: Yale University

College

Burnett School of Biomedical Sciences

Department

Molecular Biology & Microbiology

Filing Date

12-5-2007

Assignee at Filing

UCFRF

Filing Type

National Filing Record

Donated

no

Link to Patent
PDF on Google Patents

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