Related Experiment Video

Updated: Jun 20, 2026

High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies
07:10

High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies

Published on: September 29, 2023

ABC transporters as potential targets for modulation of drug resistance

L Gatti1, G L Beretta, G Cossa

  • 1Department of Experimental Oncology and Laboratories, Fondazione IRCCS Istituto Nazionale Tumori, 20133 Milan, Italy.

Mini Reviews in Medicinal Chemistry
|August 20, 2009
PubMed

Insights

ATP binding cassette transporters contribute to multidrug resistance in cancer stem cells. Inhibitors targeting these drug efflux pumps offer a promising strategy for improving antitumor therapies.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • ATP binding cassette (ABC) transporters are crucial membrane proteins involved in cellular efflux.
  • These transporters are frequently overexpressed in tumor cells, contributing to multidrug resistance (MDR).
  • ABC transporters are also recognized as potential markers for cancer stem cells (CSCs).

Purpose of the Study:

  • To provide a comprehensive overview of the functions of drug transporters.
  • To discuss the role of ATP binding cassette transporters in multidrug resistance and cancer stem cell phenotypes.
  • To explore the potential of modulating drug efflux pumps for improved cancer treatment.

Main Methods:

  • Literature review and synthesis of existing research on ABC transporters.
  • Analysis of studies investigating the role of drug efflux pumps in tumor cell resistance.
  • Examination of data on the association between ABC transporters and cancer stem cells.

Main Results:

  • ABC transporters are key mediators of multidrug resistance in various cancers.
  • Overexpression of specific ABC transporters is linked to cancer stem cell populations.
  • Modulation of these transporters presents a viable therapeutic avenue.

Conclusions:

  • Targeting ATP binding cassette transporters offers a promising strategy to overcome drug resistance in cancer.
  • Understanding transporter function and modulation is essential for developing more effective antitumor therapies.
  • Further research into specific inhibitors could lead to clinical advancements in cancer treatment.

More Related Videos

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers18:57

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

Published on: October 17, 2013

Small-Scale Plasma Membrane Preparation for the Analysis of Candida albicans Cdr1-mGFPHis09:44

Small-Scale Plasma Membrane Preparation for the Analysis of Candida albicans Cdr1-mGFPHis

Published on: June 13, 2021

Related Concept Videos

ABC Transporters: Exporter01:31

ABC Transporters: Exporter

ATP-binding cassette or ABC transporter is the largest superfamily of integral membrane proteins. The transporters have transmembrane-binding domains (TMDs) and nucleotide-binding domains (NBDs). The TMDs are specific to their substrates, whereas the NBDs are similar to engines that complete ATP hydrolysis to complete the substrate transport. They can be full transporters consisting of two TMDs and NBDs, half transporters with one TMD and NBD, while some encoded with a single TMD or NBD are...
Carrier-Mediated Transport01:06

Carrier-Mediated Transport

Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
ABC Transporters: Importer01:27

ABC Transporters: Importer

ATP-binding cassette or ABC transporters are a class of ATP-driven pumps that hydrolyze ATP to move solutes across the membrane. They can be grouped into importers and exporters. While exporters are present in all domains of life, importers exist only in bacteria and some plants.
In bacteria, based on the number of transmembrane helices and the chemical nature of their substrates, the ABC importers can be divided into three types:
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters01:16

Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

The pharmacogenetics of drug transporters is increasingly recognized as a critical factor influencing interindividual variability in drug absorption, distribution, and elimination. These membrane-bound proteins regulate drugs' movement across cellular barriers by actively pumping them out (efflux) or facilitating their uptake (influx). Among the major transporter families, ATP-binding cassette (ABC) and solute carrier (SLC) transporters play particularly prominent roles. Genetic polymorphisms...
Drug Absorption Mechanism: Carrier-Mediated Membrane Transport01:19

Drug Absorption Mechanism: Carrier-Mediated Membrane Transport

Certain large, lipid-insoluble drug molecules that resemble amino acids, peptides, or glucose, require specialized carrier proteins to facilitate their diffusion across cell membranes. This transport can occur through either facilitated diffusion, which does not require energy input, or active transport, which does require energy input.
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
Active Transport01:14

Active Transport

Active transport is a critical biological process that allows cells to move solutes against an electrochemical gradient. This process requires direct energy input and is characterized by its selectivity, saturability, and susceptibility to competitive inhibition.
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...