Targeting Wnt/β-Catenin Pathway by DNA Alkylating Pyrrole-Imidazole Polyamide in Colon Cancer.

ABSTRACT: Wnt/β-catenin pathway, which is under the control of T cell factor/lymphocyte enhancer factor (TCF/LEF) transcription factors, plays a pivotal role during carcinogenesis through the regulation of cancer cell proliferation and differentiation. Thus, it is likely that an inhibitor against this pro-oncogenic pathway might be a promising anti-cancer drug candidate. In the present study, we have synthesized a novel polyamide (WNT-Chb) composed of N-methylpyrrole, N-methylimidazole, and DNA alkylator chlorambucil, and examined its anti-cancer effect on colon cancer cells in vitro and in vivo. Based on our results, WNT-Chb preferentially bound to a consensus TCF/LEF-responsive element (5'-CCTTTGA-3'), and suppressed multiple Wnt-target gene expression. Consistent with these results, WNT-Chb atten

SUBMITTER: Shimozato O 

PROVIDER: S-EPMC12775567 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature