Recent advances in focal adhesion kinase (FAK)-targeting antitumor agents

Focal adhesion kinase (FAK) is a non-receptor intracellular tyrosine kinase that plays an important role in cell adhesion, survival, proliferation, and other processes. Research studies have shown that overexpression of FAK can promote the proliferation and migration of tumor cells. Therefore, FAK has become a promising target for small molecular anticancer drugs with great clinical potential. In recent years, research studies on small molecular FAK inhibitors have been increasing. With the rise of proteolysis-targeting chimera (PROTAC) technology, FAK PROTACs have also been developed to induce FAK degradation. This article reviews the design and biological activity of FAK-targeting antitumor agents, with a focus on their chemical structures, antitumor effects, and clinical progress.