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Updated: May 27, 2026

Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein
Published on: December 3, 2010
Multidrug resistance associated proteins in multidrug resistance
Kamlesh Sodani1, Atish Patel, Rishil J Kathawala
1Department of Pharmaceutical Sciences, St. John's University, Queens, NY 11439, USA.
Abstract:
Multidrug resistance proteins (MRPs) are members of the C family of a group of proteins named ATP-binding cassette (ABC) transporters. These ABC transporters together form the largest branch of proteins within the human body. The MRP family comprises of 13 members, of which MRP1 to MRP9 are the major transporters indicated to cause multidrug resistance in tumor cells by extruding anticancer drugs out of the cell. They are mainly lipophilic anionic transporters and are reported to transport free or conjugates of glutathione (GSH), glucuronate, or sulphate. In addition, MRP1 to MRP3 can transport neutral organic drugs in free form in the presence of free GSH. Collectively, MRPs can transport drugs that differ structurally and mechanistically, including natural anticancer drugs, nucleoside analogs, antimetabolites, and tyrosine kinase inhibitors. Many of these MRPs transport physiologically important anions such as leukotriene C4, bilirubin glucuronide, and cyclic nucleotides. This review focuses mainly on the physiological functions, cellular resistance characteristics, and probable in vivo role of MRP1 to MRP9.
Insights
Multidrug resistance proteins (MRPs), a key part of ATP-binding cassette (ABC) transporters, are crucial in cancer drug resistance. This review examines the functions and roles of MRP1-MRP9 in cellular resistance and in vivo.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Multidrug resistance proteins (MRPs) are a major subfamily of ATP-binding cassette (ABC) transporters.
- The MRP family includes 13 members, with MRP1-MRP9 primarily implicated in multidrug resistance in tumor cells.
- These transporters extrude anticancer drugs, contributing to treatment failure.
Purpose of the Study:
- To review the physiological functions of MRP1-MRP9.
- To explore the cellular resistance characteristics mediated by these transporters.
- To discuss the probable in vivo roles of MRP1-MRP9.
Main Methods:
- Literature review of existing research on MRPs.
- Analysis of studies focusing on MRP1-MRP9 functions.
- Synthesis of data on transporter substrates and resistance mechanisms.
Main Results:
- MRPs are primarily lipophilic anionic transporters, transporting glutathione (GSH), glucuronate, or sulphate conjugates.
- MRP1-MRP3 can also transport neutral organic drugs in the presence of GSH.
- These transporters exhibit broad substrate specificity, including anticancer drugs and physiological anions.
Conclusions:
- MRPs play a significant role in the efflux of diverse compounds, impacting drug efficacy and physiological processes.
- Understanding MRP functions is critical for developing strategies to overcome multidrug resistance in cancer.
- Further research into the in vivo roles of MRP1-MRP9 is warranted.
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