Profiling the kinome for drug discovery

The human kinome is made up of 518 distinctive serine/threonine and tyrosine kinases, which are key components of virtually every mammalian signal transduction pathway. Consequently, kinases provide a compelling target family for the development of small molecule inhibitors, which could be used as tools to delineate the mechanism of action for biological processes and potentially be used as therapeutics to treat human diseases such as cancer. A myriad of recent technological advances have accelerated our understanding of kinome function, its relationship to tumorigenic development, and have contributed to the progression of small molecule kinase inhibitors into the clinic. Essential to the continued growth of the field are informatics tools that can assist in interpreting disparate and voluminous data sets and correctly guide decision making processes. These advances are expected to have a dramatic impact on kinase drug development and clinical diagnoses and treatment in the near future.

Section editors:Li-He Zhang – School of Pharmaceutical Science, University of Peking, Beijing, ChinaKaixian Chen – Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China