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Multidrug Resistance and Anticonvulsants: New Studies with Some Enaminones

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The multidrug resistance (MDR), often conferred by the active extrusion of drugs from the cell, is a phenomenon often seen in cancer cells that may become resistant to a wide spectrum of drugs with varying chemical structures or cellular targets. This event has recently been reported for anticonvulsants. Studies in our laboratories on this occurrence with some enaminones have shown that the enaminones display high efflux ratios and are recognized by P-glycoprotein (P-gp) and / or the multidrug resistance protein (MRP), which have been reported as the main efflux transporters responsible for the development of MDR. Recent studies have uncovered interesting structural analogues that can modulate the functional activity of P-gp, suggesting a possible increase in the bioavailabillity of P-gp substrate drugs when administered concurrently.
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Keywords: anticonvulsants; enaminones; multidrug resistance

Document Type: Review Article

Affiliations: Department of Pharmaceutical Sciences, College of Pharmacy, Howard University, Washington, DC 20059, USA

Publication date: 01 August 2004

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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