Recent advances of β-catenin small molecule inhibitors for cancer therapy: Current development and future perspectives

Eur J Med Chem. 2022 Dec 5:243:114789. doi: 10.1016/j.ejmech.2022.114789. Epub 2022 Sep 24.

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.

Keywords: Cancer; Small molecule inhibitors; Wnt/β-catenin signaling pathway; β-catenin.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Cell Proliferation
  • Humans
  • Neoplasms* / drug therapy
  • Wnt Signaling Pathway
  • beta Catenin / metabolism

Substances

  • beta Catenin
  • Antineoplastic Agents