Drug discovery efforts toward inhibitors of canonical Wnt/β-catenin signaling pathway in the treatment of cancer: A composition-of-matter review (2010-2020)

Abstract

The Wnt/β-catenin pathway has a crucial role in the proliferation and differentiation of normal cells as well as the self-renewal and pluripotency of stem cells, including cancer stem cells (CSCs). Targeting this pathway with small-molecule chemotherapeutics, discovered via conventional efforts, has proved difficult. Recently, computer-aided drug discovery efforts have produced promising chemotherapeutics. A concerted effort to develop inhibitors of this pathway through more efficient and cost-effective drug discovery methods could lead to a significant increase in clinically relevant therapeutics. Herein, patents from 2010 to 2020 are reviewed to identify those that have disclosed composition of matter for small-molecule inhibitors of the Wnt/ β-catenin pathway for cancer. We believe that such efforts will provide insights for future therapeutic candidate discovery and development in this field.

Keywords: Anticancer; Cancer stem cells; Porcupine; Small-molecule inhibitors; Tankyrase; Wnt/β-catenin.