LL1, a novel and highly selective STAT3 inhibitor, displays anti-colorectal cancer activities in vitro and in vivo.

ABSTRACT:

Background and purpose

Signal transducer and activator of transcription 3 (STAT3) factor is associated with the development and progression of numerous types of human cancer. STAT3 activation is involved in metastasis. However, no STAT3 inhibitor has been used therapeutically. Hence, we syntheised a novel, potent and small-molecule inhibitor of STAT3, LL1, and studied its antitumour effects and investigated its mechanism of action in two tumour models.

Experimental approach

Using structure-based drug design method, based on the crystal structure of STAT3 protein, we identified a potent STAT3 inhibitor (LL1) targeting STAT3 SH2 domain and characterized its therapeutic properties and potential toxicity in vitro and in vivo using the MTT assay, colony formation assay, histologi

SUBMITTER: Liu Z 

PROVIDER: S-EPMC6989959 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature