Protein Kinase C Modulators from Marine Invertebrates
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Box 52330, 4 University Place, Durham, NC, 27717
AbstractDiscovery of new drugs depends largely upon random screening directed towards specificenzyme targets. Protein kinase C (PKC), a family of serine/threonine-specific protein kinases, is criticalin the control of multiple cellular responses, including gene expression, proliferation, differentiation andtumor promotion, and has thus become a primary target in the development of drug. Despite itsenormous therapeutic potential, only a few drug candidates that utilize the PKC pathway have beendiscovered. Recent advances in molecular biology have paved the way for expression of targetisoenzymes of P2KC in insect cells in high yields, which has enabled mass screening of samples. Marineorganisms have proven to be a very valuable source of biologically active compounds. However, theirpotential as a source for new pharmaceuticals is still largely unexplored. The primary goal of the currentproposal is to screen extracts derived from marine invertebrates in assays against isoenzymes of proteinkinase C. To represent species diversity, the marine organisms are collected from different geographicallocations. The long range objectives are to isolate and characterize small organic molecules from theseorganisms that selectively inhibit or activate protein kinase C isoenzymes and to evaluate theirtherapeutic potential.
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