Src inhibitors: genomics to therapeutics

Following the milestone discoveries that identified Src as the first known protein tyrosine kinase and as a prototype oncogene, as well as Src transge nic studies to validate it as a promising therapeutic target for osteoporos is, intense efforts are being made to create Src inhibitor drugs. Drug disc overy strategies focused on both the non-catalytic and catalytic domains of Src have successfully resulted in promising Src inhibitor lead compounds w ith potential therapeutic applications for osteoporosis, cancer, and other diseases. Some noteworthy examples of Src inhibitors are described, and the ir chemical diversity, structure-based design, and biological activities in vitro and in vivo are illustrated. The potency, selectivity, and in vivo e fficacy of key Src inhibitors are being investigated in molecular, cellular and animal models. Consequently, Src inhibitor drug development is imminen t, and current studies are well-poised to achieve the ultimate milestone of a Src inhibitor therapeutic.