Related Experiment Video

Updated: Mar 17, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
10:28

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers

Published on: September 20, 2018

7.0K

ATP-binding cassette transmembrane transporters and their epigenetic control in cancer: an overview

Elena Arrigoni1, Sara Galimberti2, Mario Petrini2

  • 1a Section of Pharmacology, Department of Clinical and Experimental Medicine , University of Pisa , Pisa , Italy.

Expert Opinion on Drug Metabolism & Toxicology
|July 27, 2016
PubMed
Abstract

Insights

Epigenetic mechanisms like DNA methylation and histone modifications regulate ATP-binding cassette (ABC) transporters. This control influences multidrug resistance (MDR) phenotype, impacting cancer treatment outcomes.

Area of Science:

  • Molecular Biology
  • Pharmacology
  • Cancer Research

Background:

  • ATP-binding cassette (ABC) transporters regulate drug passage across cell membranes, influencing drug pharmacokinetics and pharmacodynamics.
  • These transporters are implicated in the multidrug resistance (MDR) phenotype, a major challenge in cancer chemotherapy.
  • While pharmacogenetics offers insights, a significant portion of drug response variability remains unexplained.

Purpose of the Study:

  • To review the epigenetic mechanisms controlling ABC transporter gene expression.
  • To explore the association between epigenetic modifications and the MDR phenotype in human cancer.
  • To discuss the clinical implications of epigenetic regulation of ABC transporters for therapeutic outcomes.

Main Methods:

  • Review of literature on epigenetic mechanisms including DNA methylation and histone modifications.
  • Analysis of the role of noncoding RNAs in post-transcriptional control of ABC transporters (ABCB1, ABCC1, ABCG2).
  • Examination of the link between epigenetic regulation and MDR phenotype in cancer.

Main Results:

  • Epigenetic mechanisms, including DNA methylation, histone modifications (acetylation, methylation, phosphorylation), and noncoding RNAs, significantly impact ABC transporter gene expression.
  • These epigenetic alterations are closely associated with the development and maintenance of the MDR phenotype in various human cancers.
  • Specific ABC transporters (ABCB1, ABCC1, ABCG2) are key targets of this epigenetic control.

Conclusions:

  • Epigenetic regulation plays a crucial role in controlling ABC transporter activity and the MDR phenotype.
  • Understanding these epigenetic mechanisms is vital for predicting and overcoming drug resistance in cancer therapy.
  • Further investigation into the clinical applications of targeting epigenetic control of ABC transporters is warranted.
Keywords:
ABC transportersEpigeneticsMDRcancerepigenomics

More Related Videos

ATAC-Seq Optimization for Cancer Epigenetics Research07:13

ATAC-Seq Optimization for Cancer Epigenetics Research

Published on: June 30, 2022

5.5K
Methods to Discover Alternative Promoter Usage and Transcriptional Regulation of Murine Bcrp111:02

Methods to Discover Alternative Promoter Usage and Transcriptional Regulation of Murine Bcrp1

Published on: May 27, 2016

8.6K

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...
7.0K
Epigenetic Regulation01:37

Epigenetic Regulation

Epigenetic changes alter the physical structure of the DNA without changing the genetic sequence and often regulate whether genes are turned on or off. This regulation ensures that each cell produces only proteins necessary for its function. For example, proteins that promote bone growth are not produced in muscle cells. Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
X-chromosome...
4.1K
Epigenetic Regulation01:46

Epigenetic Regulation

Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
34.2K
Epigenetic Regulation01:46

Epigenetic Regulation

26.2K
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:
3.7K
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...
95