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Updated: Aug 27, 2025

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Published on: June 17, 2014
Recent advances of β-catenin small molecule inhibitors for cancer therapy: Current development and future
Panpan Yang1, Yumeng Zhu1, Qinwen Zheng1
1Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu, 610041, China.
Abstract:
The Wnt/β-catenin signaling pathway is involved in many cellular physiological processes, including embryonic development, cell proliferation and differentiation, tissue homeostasis and regeneration, etc. Aberrant activation of Wnt/β-catenin signaling is one of the most typical features in the development and progression of cancer. Abnormal accumulation of β-catenin, a core component of the Wnt/β-catenin signaling pathway, is one of the main factors leading to abnormal activation of the Wnt/β-catenin signaling pathway. Therefore, β-catenin has become an important target for the development of anticancer drugs. Some β-catenin small molecule inhibitors have been shown to have the potential to treat cancer, such as the specific β-catenin/CBP antagonist PRI-724, which has entered phase I/II clinical trials. However, the development and application of β-catenin inhibitors are still challenging due to their selectivity, specificity and physicochemical properties, etc. This review introduces the Wnt/β-catenin signaling pathway, focuses on the research progress of β-catenin small molecule inhibitors, and prospects for the development of drug in the future.
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