Creating chemical diversity to target protein kinases.
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.
Department of Biological Chemistry, Genomics Institute of the Novartis Research Foundation, San Diego, CA 92121, USA.
B
B
Li
Y
Y
Liu
T
T
Uno
N
N
Gray
D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008968:Molecular Conformation; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000737:chemistry; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases