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.

P-glycoprotein (P-gp, ABCB1, MDR1) is a well-characterized 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. Due to the role of P-gp in extruding xenobiotics from a broad range of cells, this transporter also confers the multidrug resistance phenotype in many different cell types.

Members of the multidrug resistance protein (MRP) family and P-gp also help maintain the integrity of the blood-brain-barrier, often preventing the entry of drugs or removing them from the CNS. This can pose a problem in therapies for CNS disorders, particularly the treatment of brain tumors.

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-stabilizing drug taxol.

External sources of pharmacological information for Multidrug Transporters :

• BJP Guide

Literature for Multidrug Transporters

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Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

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Multidrug Transporter Gene Data