Hitting the Right Kinase Targets Protein Kinase Selection for Drug Discovery

摘要

Only ～15% of the 515 human protein kinases have been targeted for drug discovery and primarily for cancer treatment. Over 150 therapeutics against kinases have been tested in the clinic and 16 have received market approval, but most of these kinase inhibitors have limited specificity. Furthermore, much of the R&D effort in this area is misplaced on critical kinase targets that are ubiquitous in human tissues and highly conserved in diverse species.