At first glance, the odds that the introduction of a diminutive and unsuspicious phosphoryl group on to a hydroxycontaining side chain of a much larger protein molecule would be selected by Nature as the most widely deployed mechanism to control biological processes, and be responsible for many major diseases, seems unlikely. However, this process termed protein phosphorylation is a vital regu lator of almost all events that take place in eukaryotic organisms. In this review we will outline what phosphorylation is, how it is regulated and why disruptions of the network of enzymes and proteins that regulate the phosphorylation are a principal cause of many maladies. We will also discuss how advances are leading to exciting strategies to develop drugs to treat diseases caused by disruptions of protein phosphorylation.

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