Multidrug Transporters

Supporting information

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.

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
ABCA1 Human ABCA1 NM_005502 Q9UN09
Mouse Abca1 NM_013454 P41233
Rat Abca1 NM_178095 Q80ZB2
ABCA2 Human ABCA2 NM_001606 Q9BZC7
Mouse Abca2 NM_007379 P41234
Rat Abca2 NM_024396 Q9ESR9
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Literature for Multidrug Transporters

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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Cancer Research Product Guide
Programmed Cell Death Life Science Poster

Written by Bram van Raam & Guy Salvesen, 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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Programmed Cell Death Life Science Poster

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Cancer Research Product Guide

Cancer Research Product Guide

Our Cancer Research Guide highlights over 750 products for cancer research. Request copy or view PDF today.

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Programmed Cell Death

Written by Bram van Raam and Guy Salvesen

Programmed Cell Death Life Science Poster

Our Programmed Cell Death poster gives a summary of the signaling pathways involved in apoptosis, necroptosis and cell survival. Request copy or view PDF today.

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