Novel chemical genetic approaches to the discovery of signal transduction inhibitors.
Concurrent advances in both high-throughput chemistry and genomics have given rise to the field of chemical genetics as a discipline for elucidating and validating drug targets, and generating novel therapeutics. Indeed, chemical genetic approaches to drug discovery have now been applied to several important drug target classes, especially those involved in signal transduction. Chemical genetics is distinct from the broader term "chemogenomics" which is defined as the description of all possible drugs against all possible targets (reviewed in [1]). This review covers several "orthogonal" chemical genetic approaches and focuses on a unique analog sensitive kinase technology and its applications to kinase drug discovery.
Shokat
Kevan
K
Dept of Cellular and Molecular Pharmacology, University of California at San Francisco, San Francisco, CA, USA.
Velleca
Mark
M
D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D008967:Molecular Biology; D010770:Phosphotransferases / Q000037:antagonists & inhibitors / Q000235:genetics; D015398:Signal Transduction / Q000187:drug effects* / Q000235:genetics*
D004791:Enzyme Inhibitors; D010770:Phosphotransferases