Profiling the kinome for drug discovery

S Frank Yan; Frederick J King; Yingyao Zhou; Markus Warmuth; Gang Xia

doi:10.1016/j.ddtec.2006.09.012

Profiling the kinome for drug discovery

Drug Discov Today Technol. 2006 Autumn;3(3):269-76. doi: 10.1016/j.ddtec.2006.09.012.

Authors

S Frank Yan¹, Frederick J King², Yingyao Zhou¹, Markus Warmuth³, Gang Xia⁴

Affiliations

¹ Cheminformatics, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
² Developmental and Molecular Pathways, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
³ Kinase Drug Discovery, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA. Electronic address:mwarmuth@gnf.org.
⁴ Kinase Drug Discovery, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA. Electronic address:gxia@gnf.org.

PMID: 24980528
DOI: 10.1016/j.ddtec.2006.09.012

Abstract

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.: