Discovery of small molecule inhibitors of the Wnt/β-catenin signaling pathway by targeting β-catenin/Tcf4 interactions

作者：Yan, Maocai; Li, Guanqun; An, Jing^*

来源：Experimental Biology and Medicine, 2017, 242(11): 1185-1197.

DOI：10.1177/1535370217708198

• beta-Catenin
• Tcf4
• small molecule inhibitors
• Wnt/beta-catenin signaling pathway
• protein-protein interactions
• anticancer agents

The Wnt/beta-catenin signaling pathway typically shows aberrant activation in various cancer cells, especially colorectal cancer cells. This signaling pathway regulates the expression of a variety of tumor-related proteins, including c-myc and cyclin D1, and plays essential roles in tumorigenesis and in the development of many cancers. Small molecules that block the interactions between -catenin and Tcf4, a downstream stage of activation of the Wnt/beta-catenin signaling pathway, could efficiently cut off this signal transduction and thereby act as a novel class of anticancer drugs. This paper reviews the currently reported inhibitors that target beta-catenin/Tcf4 interactions, focusing on the discovery approaches taken in the design of these inhibitors and their bioactivities. A brief perspective is then shared on the future discovery and development of this class of inhibitors.

• 出版日期2017-6
• 单位济宁医学院