Physiological functions of protein kinase inhibitors.
Protein kinases are key regulatory enzymes involved in a multitude of biochemical pathways. This chapter will describe the current research on targeting specific protein kinases with inhibitors in attempts to disrupt flux through specific pathways. Targeting specific kinases presents a distinct challenge as there are hundreds of individual kinase enzymes that use ATP as a substrate to phosphorylate specific target molecules. The challenge clearly lies in obtaining specificity for a given kinase, thus allowing inhibition or activation of a specific pathway. This chapter will focus on two areas of kinase inhibitors, those that target the MAP kinase pathway and those directed against the phosphatidylinositol-3 kinase (PI-3K) related kinase family. The cellular and physiological effects of inhibition of the various pathways controlled by these kinases will be reviewed.
Turchi
J J
JJ
Department of Biochemistry and Molecular Biology, Wright State University School of Medicine, Dayton, Ohio 45435, USA.
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D000730:Androstadienes / Q000494:pharmacology; D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D020928:Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors / Q000502:physiology; D016328:NF-kappa B / Q000037:antagonists & inhibitors / Q000502:physiology; D019869:Phosphatidylinositol 3-Kinases / Q000502:physiology; D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000502:physiology; D015398:Signal Transduction; D020123:Sirolimus / Q000494:pharmacology; D000077191:Wortmannin
D000730:Androstadienes; D004791:Enzyme Inhibitors; D020928:Mitogen-Activated Protein Kinases; D016328:NF-kappa B; D019869:Phosphatidylinositol 3-Kinases; D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases; D020123:Sirolimus; D000077191:Wortmannin