2. Academic Validation
  3. Is β-Catenin a Druggable Target for Cancer Therapy?

Is β-Catenin a Druggable Target for Cancer Therapy?

  • Trends Biochem Sci. 2018 Aug;43(8):623-634. doi: 10.1016/j.tibs.2018.06.003.
Can Cui 1,  Xianglian Zhou 1,  Weidong Zhang 2,  Yi Qu 3,  Xisong Ke 4
Affiliations

Affiliations

  • 1 Innovation Center of Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, China; These authors contributed equally to the manuscript.
  • 2 Innovation Center of Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, China; School of Pharmacy, Second Military Medical University, Shanghai, China. Electronic address: [email protected].
  • 3 Innovation Center of Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, China. Electronic address: [email protected].
  • 4 Innovation Center of Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, China. Electronic address: [email protected].
PMID: 30056837 DOI: 10.1016/j.tibs.2018.06.003
Abstract

Mutations of canonical Wnt signaling pathway genes frequently occur in Cancer and lead to abnormal accumulation of the key effector β-catenin. Over the past decades, a number of Wnt inhibitors have been identified through high-throughput screenings, however, very few of them target β-catenin directly, raising questions regarding its druggability. Here, we review Wnt inhibitors with a focus on small molecules that directly bind β-catenin, discuss the druggability of β-catenin, and why it has rarely been targeted, especially in the cellular context. We also propose strategies to develop small molecule binding and depleting cellular β-catenin, which are generally applicable to Other difficult-to-drug or yet-to-be-drugged targets.

Keywords

cancer; druggability; interaction in vivo; intrinsically disordered protein region; protein depletion; β-catenin.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-122649
    99.88%, β-catenin Inhibitor