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>Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1.
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Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1.
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机译：Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1.
The multidrug resistance protein 1 (MRP1), involved in multidrug resistance (MDR) of cancer cells, was found to be modulated by verapamil, through stimulation of GSH transport, leading to apoptosis of MRP1-overexpressing cells. In this study, various iodinated derivatives of verapamil were synthesized, including iodination on the B ring, known to be involved in verapamil cardiotoxicity, and assayed for the stimulation of GSH efflux by MRP1. The iodination, for nearly all compounds, led to a higher stimulation of GSH efflux. However, determination of concomitant cytotoxicity is also important for selecting the best compound, which was found to be 10-fold more potent than verapamil. This will then allow us to design original anti-cancer compounds which could specifically kill the resistant cancer cells.
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