Protein kinases and phosphatases as therapeutic targets in cancer

RESUMEN

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ABSTRACT

Protein phosphorylation plays key roles in many physiologicalprocesses and is often deregulated in pathologicalconditions. Our current understanding of howprotein kinases and phosphatases orchestrate thephosphorylation changes that control cellular functionshas made these enzymes potential drug targetsfor the treatment of many diseases. The success of thetyrosine kinase inhibitor Gleevec in the treatment ofsome cancers has further invigorated the developmentof kinase inhibitors as anti-cancer drugs. Alarge number of these compounds are currently undergoingclinical trials and there is much expectationon the therapeutic potential of these molecules, asmore specific and less toxic drugs than currentlyused generic chemotherapeutic agents. In this manuscript,we review the current status of more than 30protein kinase inhibitors with proven or potentialtherapeutic value for cancer treatment. These includeinhibitors of receptor and cytosolic tyrosine kinasesas well as compounds that target different families ofserine/threonine kinases involved in signalling andcell cycle regulation. We also briefly touch on theprospects of phosphatase inhibitors. The combinationof kinase inhibitors to target different components ofsignalling pathways that are found deregulated in tumoursis also emerging as an interesting approach forcancer therapy