Multidrug Transporters

ATP-binding cassette (ABC) transporters form one of the largest groups of paralogous protein families that have a wide diversity of functions and substrates. Specificity has been shown for small and large molecules, highly charged molecules and highly hydrophobic molecule systems such as that for polysaccharides. Multidrug transporters (MDRs) are a specific type of ABC transporter and are commonly overexpressed in cancer cells.

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P-Glycoprotein

P-glycoprotein (ABCB1, MDR1) is a well-characterised human ABC transporter that was the first ABC transporter implicated in multidrug resistance. Normal physiological expression of P-glycoprotein has been found to prevent uptake of some lipophilic drugs into the brain and other key organs. P-glycoprotein is frequently overexpressed in cancer cells resulting in drugs being pumped out of the cells faster than they can enter. This causes a lower concentration of the drug in the cell and reduces the effectiveness of the drugs in killing cancer cells. Drugs that are affected by classical multidrug resistance include the vinca alkaloids (vinblastine and vincristine), the anthracyclines (doxorubicin and daunorubicin), the RNA transcription inhibitor actinomycin D and the microtubule-stabilising drug taxol.

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Cancer Research Product Guide

Cancer Research Product Guide

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