Aberrant accumulation of beta-catenin in the cell nucleus as a result of deregulation of the Wnt/beta-catenin pathway is found in various types of cancer. Direct beta-catenin targeting agents are being researched despite obstacles; however, specific beta-catenin drugs for clinical treatments have not been approved so far. We focused on direct beta-catenin targeting of potential therapeutic value as anticancer agents. This review provides recent advances on small molecule beta-catenin agents. Structure-activity relationships and biological activities of reported inhibitors are discussed. This work provides useful knowledge in the discovery of beta-catenin agents.
Nalli, M., Masci, D., Urbani, A., La Regina, G., Silvestri, R., Emerging Direct Targeting β-Catenin Agents, <<MOLECULES>>, 2022; 27 (22): 1-15. [doi:10.3390/molecules27227735] [https://hdl.handle.net/10807/268797]
Emerging Direct Targeting β-Catenin Agents
Masci, DomizianaSecondo
;Urbani, Andrea;La Regina, Giuseppe;
2022
Abstract
Aberrant accumulation of beta-catenin in the cell nucleus as a result of deregulation of the Wnt/beta-catenin pathway is found in various types of cancer. Direct beta-catenin targeting agents are being researched despite obstacles; however, specific beta-catenin drugs for clinical treatments have not been approved so far. We focused on direct beta-catenin targeting of potential therapeutic value as anticancer agents. This review provides recent advances on small molecule beta-catenin agents. Structure-activity relationships and biological activities of reported inhibitors are discussed. This work provides useful knowledge in the discovery of beta-catenin agents.
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