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.
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