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Drug resistance involves multiple mechanisms.Multidrug resistance (MDR) is the leading cause of treatment failure in cancer therapy.Elevated levels of MDR proteins [members of the ATP-binding cassette (ABC) transporter family] increase cellular efflux and decrease the effectiveness of chemotherapeutic agents.As a salvage approach to overcome drug resistance, inhibitors of MDR proteins have been developed, but have had limited success mainly due to undesired toxicities.