Related Experiment Video
Updated: Jun 18, 2026

Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein
Published on: December 3, 2010
Molecular mechanism of ATP-dependent solute transport by multidrug resistance-associated protein 1
1Mayo Clinic College of Medicine, Mayo Clinic Arizona, Scottsdale, AZ, USA. xbchang@mayo.edu
Abstract:
Millions of new cancer patients are diagnosed each year and over half of these patients die from this devastating disease. Thus, cancer causes a major public health problem worldwide. Chemotherapy remains the principal mode to treat many metastatic cancers. However, occurrence of cellular multidrug resistance (MDR) prevents efficient killing of cancer cells, leading to chemotherapeutic treatment failure. Over-expression of ATP-binding cassette transporters, such as P-glycoprotein, breast cancer resistance protein and/or multidrug resistance-associated protein 1 (MRP1), confers an acquired MDR due to their capabilities of transporting a broad range of chemically diverse anticancer drugs across the cell membrane barrier. In this review, the molecular mechanism of ATP-dependent solute transport by MRP1 will be addressed.
Insights
Multidrug resistance (MDR) in cancer hinders chemotherapy effectiveness. This review details the molecular mechanism of ATP-dependent solute transport by the MRP1 transporter, a key factor in MDR.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Cancer is a significant global health issue, with chemotherapy being a primary treatment for metastatic cancers.
- Cellular multidrug resistance (MDR) frequently leads to treatment failure by preventing effective cancer cell killing.
- ATP-binding cassette transporters, including MRP1, are implicated in acquired MDR through their drug efflux capabilities.
Purpose of the Study:
- To elucidate the molecular mechanisms underlying ATP-dependent solute transport mediated by the Multidrug Resistance-Associated Protein 1 (MRP1).
- To provide a comprehensive review of MRP1's role in conferring cellular multidrug resistance.
Main Methods:
- Literature review focusing on molecular mechanisms of MRP1.
- Analysis of studies detailing ATP-dependent solute transport processes.
- Examination of MRP1's interaction with anticancer drugs.
Main Results:
- MRP1 utilizes ATP hydrolysis to actively transport a diverse range of anticancer drugs out of cells.
- Over-expression of MRP1 is a significant contributor to acquired cellular multidrug resistance.
- Understanding MRP1's transport mechanism is crucial for overcoming chemotherapy resistance.
Conclusions:
- MRP1-mediated drug efflux is a critical mechanism driving chemotherapy resistance in cancer.
- Targeting MRP1 function may offer strategies to improve chemotherapeutic efficacy.
- Further research into MRP1's molecular transport is warranted for clinical applications.
Related Concept Videos
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Active Transport
Primary active transporters, like Na+, K+ and -ATPase, directly utilize ATP to move ions across the membrane. These transporters play significant roles in various physiological processes. For instance, Na+, K+ and -ATPase maintain...
Membrane Transporters
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
ABC Transporters: Exporter
ATP Driven Pumps I: An Overview
There are four main types of ATP-driven pumps - P-type, V-type, F-type, and ABC transporter. All these pumps are of varying complexities and are...
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

