[Protein kinase C as a potential target for drug development in cancer  research].
The central role of protein kinase C (PKC) in cellular signaling makes it an attractive and promising target for drug development. With increasing insight into the regulation by ligands, by phosphorylation, and by macromolecular interactions involved in localization, we will be able to predict the consequences of modifications in second messenger levels resulting from changes in oncogenes, growth factors, or the exposures to xenobiotics. The multiplicity of functionally distinct isoforms of PKC and the depth of modification of their properties in a cell-context specific fashion provide abundant opportunities for generating therapeutic specificity. The emerging elucidation of the complexities of regulation of PKC folding and localization presents the opportunity to pursue novel strategies for intervention, complementing the efforts directed at the design of selective catalytic site inhibitors. Although PKC initially attracted the attention of cancer researchers as a potential therapeutic target, its general role in signal transduction affords a much broader field of opportunity.
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Molecular Mechanisms of Tumor Promotion Section, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA.
Paragh
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D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000187:drug effects* / Q000378:metabolism*
D000970:Antineoplastic Agents; D011493:Protein Kinase C