Recent advances in novel anticancer agents targeting β-catenin/TCF4 interaction for molecular cancer therapeutics
10.16438/j.0513-4870.2021-0018
- VernacularTitle:靶向β-catenin/TCF4相互作用抑制剂在肿瘤分子治疗中的研究进展
- Author:
Zheng-hao FU
;
Gan-gan YAN
;
Hai-yan QI
;
Xiao-ping LIU
;
Yun-yu CHEN
- Publication Type:Research Article
- Keywords:
Wnt inhibitor;
italic>β-catenin/TCF4 interaction;
italic>β-catenin/LEF1 interaction;
protein-protein interaction;
anticancer activity
- From:
Acta Pharmaceutica Sinica
2021;56(5):1238-1245
- CountryChina
- Language:Chinese
-
Abstract:
Wnt/β-catenin signaling pathway plays an important role in the proliferation, growth, invasion, and metastasis of human cancers. Moreover, β-catenin/T-cell factor 4 (TCF4) interaction regulates the transcription of the key oncogenes in Wnt/β-catenin signaling pathway. Therefore, β-catenin/TCF4 interaction would be a promising therapeutic target for the development of highly selective anticancer agents. At present, most ongoing small-molecule inhibitors targeting β-catenin/TCF4 interaction, including PKF222-815, iCRT3/5/14, LF3, and sanguinarine, have been developed in preclinical studies for human cancer therapeutics. In this review, we summarized the research advances of up-to date inhibitors targeting β-catenin/TCF4 interaction, including the molecular structure and cellular functions of β-catenin in canonical Wnt signaling pathway. This review holds a hopeful avenue for the development of novel and highly selective Wnt inhibitors targeting β-catenin/TCF4 interaction for future anticancer strategy.
