Related Experiment Video
Updated: Nov 19, 2025

Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein
Published on: December 3, 2010
Multidrug resistance proteins (MRPs): Structure, function and the overcoming of cancer multidrug resistance
Jing-Quan Wang1, Yuqi Yang1, Chao-Yun Cai1
1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA.
Abstract:
ATP-binding cassette (ABC) transporters mediate the ATP-driven translocation of structurally and mechanistically distinct substrates against steep concentration gradients. Among the seven human ABC subfamilies namely ABCA-ABCG, ABCC is the largest subfamily with 13 members. In this respect, 9 of the ABCC members are termed "multidrug resistance proteins" (MRPs1-9) due to their ability to mediate cancer multidrug resistance (MDR) by extruding various chemotherapeutic agents or their metabolites from tumor cells. Furthermore, MRPs are also responsible for the ATP-driven efflux of physiologically important organic anions such as leukotriene C4, folic acid, bile acids and cAMP. Thus, MRPs are involved in important regulatory pathways. Blocking the anticancer drug efflux function of MRPs has shown promising results in overcoming cancer MDR. As a result, many novel MRP modulators have been developed in the past decade. In the current review, we summarize the structure, tissue distribution, biological and pharmacological functions as well as clinical insights of MRPs. Furthermore, recent updates in MRP modulators and their therapeutic applications in clinical trials are also discussed.
Insights
Multidrug resistance proteins (MRPs) are key in cancer drug resistance by extruding chemotherapy. Novel MRP modulators show promise in overcoming this resistance, offering new therapeutic avenues.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- ATP-binding cassette (ABC) transporters facilitate ATP-driven substrate translocation.
- The ABCC subfamily, particularly multidrug resistance proteins (MRPs 1-9), plays a crucial role in cancer multidrug resistance (MDR).
- MRPs also efflux vital organic anions, impacting regulatory pathways.
Purpose of the Study:
- To review the structure, distribution, functions, and clinical relevance of MRPs.
- To discuss recent advancements in MRP modulators and their therapeutic applications.
- To highlight the potential of targeting MRPs for overcoming cancer MDR.
Main Methods:
- Literature review of scientific publications on MRPs.
- Analysis of data on MRP structure, tissue distribution, and biological functions.
- Synthesis of information on pharmacological properties and clinical trial outcomes of MRP modulators.
Main Results:
- MRPs are implicated in both cancer MDR and the transport of essential organic anions.
- Inhibiting MRPs' drug efflux function is a viable strategy against cancer MDR.
- Numerous novel MRP modulators have been developed and are under investigation.
Conclusions:
- MRPs are critical targets for cancer therapy due to their role in MDR.
- Targeting MRPs with novel modulators offers a promising approach to improve chemotherapy efficacy.
- Further research and clinical trials are essential to fully realize the therapeutic potential of MRP modulators.
More Related Videos
08:59Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down
Published on: December 11, 2017
08:46Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
Published on: December 9, 2015
Related Concept Videos
Treatment Resistant Cancers
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
ABC Transporters: Exporter
Mismatch Repair
Mismatch Repair
The Mutator Protein Family Plays a Key Role in DNA Mismatch Repair
The human genome has more than 3 billion base pairs of DNA per cell. Prior to cell division, that vast amount of genetic...
Targeted Cancer Therapies
There are several types of targeted therapies against...