An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer.

ABSTRACT: Signal transducer and activator of transcription 3 (STAT3) remains a challenging and attractive therapeutic target in cancer research. The coiled-coil domain (CCD) of STAT3 represents a novel site for targeted intervention, distinct from the Src-homology 2 domain, and plays a crucial role in regulating the earlier activation and biological function of STAT3 in cell proliferation, survival and invasion of breast cancer cells. We previously reported K116, N'-(1-(2,4-dihydroxyphenyl)ethylidene)thiophene-2-carbohydrazide, as a potent allosteric inhibitor specifically targeting the STAT3 CCD. This study aimed to investigate the antiproliferation effect of K116 on breast cancer cells in vitro and in vivo. The results showed that K116 inhibited the proliferation of breast can

SUBMITTER: Huang M 

PROVIDER: S-EPMC11969721 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature