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Updated: Apr 15, 2026

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
Published on: December 9, 2015
Multidrug Resistance Proteins (MRPs) and Cancer Therapy
Yun-Kai Zhang1, Yi-Jun Wang, Pranav Gupta
1College of Pharmacy and Health Sciences, St. John's University, 8000 Utopia Parkway, Queens, NY, 11439, USA, yunkai.zhang12@stjohns.edu.
Abstract:
The ATP-binding cassette (ABC) transporters are members of a protein superfamily that are known to translocate various substrates across membranes, including metabolic products, lipids and sterols, and xenobiotic drugs. Multidrug resistance proteins (MRPs) belong to the subfamily C in the ABC transporter superfamily. MRPs have been implicated in mediating multidrug resistance by actively extruding chemotherapeutic substrates. Moreover, some MRPs are known to be essential in physiological excretory or regulatory pathways. The importance of MRPs in cancer therapy is also implied by their clinical insights. Modulating the function of MRPs to re-sensitize chemotherapeutic agents in cancer therapy shows great promise in cancer therapy; thus, multiple MRP inhibitors have been developed recently. This review article summarizes the structure, distribution, and physiological as well as pharmacological function of MRP1-MRP9 in cancer chemotherapy. Several novel modulators targeting MRPs in cancer therapy are also discussed.
Insights
Multidrug resistance proteins (MRPs) are key in cancer therapy by extruding chemotherapy drugs. Inhibiting MRPs shows promise for resensitizing cancer cells to chemotherapy, offering new treatment strategies.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- ATP-binding cassette (ABC) transporters are crucial for membrane transport.
- Multidrug resistance proteins (MRPs) are an ABC transporter subfamily involved in drug efflux.
- MRPs contribute to multidrug resistance in cancer chemotherapy.
Purpose of the Study:
- To review the structure, distribution, and functions of MRP1-MRP9.
- To discuss the role of MRPs in cancer chemotherapy.
- To highlight novel modulators targeting MRPs for cancer therapy.
Main Methods:
- Literature review of scientific articles on MRPs.
- Analysis of physiological and pharmacological roles of MRPs.
- Summary of current research on MRP inhibitors.
Main Results:
- MRPs actively extrude chemotherapeutic agents, leading to drug resistance.
- Some MRPs play essential roles in normal physiological processes.
- Modulating MRP function can re-sensitize cancer cells to chemotherapy.
Conclusions:
- MRPs are significant targets in cancer therapy.
- Developing MRP inhibitors is a promising strategy to overcome drug resistance.
- Further research into MRP modulators could enhance chemotherapy efficacy.
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