Creating Chemical Diversity to Target Protein Kinases
B. Li, Y. Liu, T. Uno and N. Gray
Affiliation: Department of Biological Chemistry, Genomics Institute of the Novartis Research Foundation, 10675John Jay Hopkins Drive, San Diego, CA 92121, USA.
Keywords: kinase inhibitors, protein kinases, protein phosphorylation, signal transduction, kinase-targeted libraries, anticancer drugs, anti-inflammatory drugs
Protein kinases play crucial roles in regulating virtually every cellular process and are currently attracting tremendous interest as drug targets from the pharmaceutical industry. The major challenges facing the development of the potential kinase inhibitor drugs are: selectivity, physical properties (solubility, molecular weight), and pharmacological properties (bioavailability, half life, toxicity, etc.) This review focuses on how selective protein kinase inhibitors that target the ATP and allosteric binding sites are currently being identified and optimized.
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