Friday November 27 2009 | Biotechnology feed | All feeds
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Friday November 27 2009 | Biotechnology feed | All feeds
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Predicting p-glycoprotein inhibitors A variety of chemotherapies are available to oncologists and these generally reduce the rate of tumor progression. However intrinsic or acquired tumor-mediated drug resistance is a major clinical obstacle that can result in the lack of tumor responsiveness in patients undergoing treatment. Drug resistance is in part due to active efflux transporters such as p-glycoprotein. More recently data has suggested that p-glycoprotein is also involved in the passage of molecules across the blood brain barrier, and in inducing apoptosis in peripheral blood mononuclear cells. The development of substrates or inhibitors of this protein therefore represents an active area of the pharmaceutical industry. Indeed at least 19 molecules are in development, over half of which are in preclinical phases of evaluation. The identification of novel classes of p-glycoprotein ligands remains a priority and the development of in silico screening tools should help speed this process. It is therefore of interest that Eli Lilly researchers have recently determined 3-D structure-activity relationships for families of p-glycoprotein ligands and from this they have now established a model that can accurately predict p-glycoprotein interaction. This screen should be important not only for the development of anti-cancer molecules, but it may also lead to improved treatments of CNS and inflammatory disorders. Link to journal abstract:
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