Targeting the human kinome for cancer therapy: current perspectives

Abstract

As highlighted by other articles in this review issue, great progress has been made in the development of targeted treatment modalities directed against particular oncogenic kinases, and the translation of these therapies into the clinic. However, recent data from cancer genome sequencing projects indicate that the spectrum of kinases that contribute to cancer progression is wider than previously imagined, and as international projects in this area gather momentum, it appears likely that further kinase oncogenes will be identified, and the roles of previously characterized ones will be extended to subsets of additional cancers. In addition, complementary approaches such as functional genomics and mass spectrometry (MS)-based proteomics are providing important insights into the functional roles played by specific kinases in particular cancers, the dependency of these roles on genetic background, how altered kinase regulation perturbs intracellular signaling networks, and how the latter respond to targeted agents that target the kinase in question. While other articles in this issue focus on individual cancer-associated kinases and their therapeutic targeting, the aim of this review is to take a broader perspective regarding our current knowledge of the cancer kinome and how this can be expanded and exploited for clinical utility.