Recent advances of small-molecule c-Src inhibitors for potential therapeutic utilities.

Proto-oncogene tyrosine-protein kinase Src, also known as c-Src, belongs to the family of non-receptor tyrosine protein kinases (TKs) called Src kinases. It plays a crucial role in cell division, motility, adhesion, and survival in both normal cells and cancer cells by activating various signaling pathways mediated by multiple cytokines. Additionally, c-Src kinase has been implicated in osteoclasts and bone loss diseases mediated by inflammation and osteoporosis. In recent years, remarkable advancements have been achieved in the development of c-Src inhibitors, with several candidates progressing to the clinical stage. This review focuses on the research progress in several areas, including the mechanism of action, drug discovery, combination therapy, and clinical research. By presenting this information, we aim to provide researchers with convenient access to valuable insights and inspire new ideas to expedite future drug discovery programs.