Abstract
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.
Keywords: multidrug resistance, anticonvulsants, enaminones
Current Medicinal Chemistry
Title: Multidrug Resistance and Anticonvulsants: New Studies with Some Enaminones
Volume: 11 Issue: 15
Author(s): Noha Nabil Salama, Natalie D. Eddington, Debra Payne, Tiffany L. Wilson and K. R. Scott
Affiliation:
Keywords: multidrug resistance, anticonvulsants, enaminones
Abstract: 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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Cite this article as:
Salama Nabil Noha, Eddington D. Natalie, Payne Debra, Wilson L. Tiffany and Scott R. K., Multidrug Resistance and Anticonvulsants: New Studies with Some Enaminones, Current Medicinal Chemistry 2004; 11 (15) . https://dx.doi.org/10.2174/0929867043364766
DOI https://dx.doi.org/10.2174/0929867043364766 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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