Related Experiment Video

Updated: May 23, 2026

Methods to Discover Alternative Promoter Usage and Transcriptional Regulation of Murine Bcrp1
11:02

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

Published on: May 27, 2016

Human ABCG2: structure, function, and its role in multidrug resistance

Wei Mo1, Jian-Ting Zhang

  • 1Department of Pharmacology and Toxicology and IU Simon Cancer Center, Indiana University School of Medicine Indianapolis, IN 46202, USA.

International Journal of Biochemistry and Molecular Biology
|April 18, 2012
PubMed

Insights

Targeting the stability of human ATP-binding cassette (ABC) transporter ABCG2 offers a novel strategy against multidrug resistance (MDR) in cancer. Modulating ABCG2 biogenesis can reduce its levels, potentially sensitizing resistant cancers to chemotherapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Human ATP-binding cassette (ABC) transporter ABCG2 is implicated in multidrug resistance (MDR) in cancer chemotherapy.
  • ABCG2 plays a role in protecting cancer stem cells and possesses a complex oligomeric structure.
  • The biogenesis of ABCG2 can be modulated by small molecule compounds.

Purpose of the Study:

  • To review recent advancements in understanding the structure and function of ABCG2.
  • To explore the biogenesis of ABCG2 and its modulation by small molecules.
  • To discuss the physiological and pathophysiological roles of ABCG2, particularly in cancer.

Main Methods:

  • Literature review of recent studies on ABCG2.
  • Analysis of research on small molecule modulators of ABCG2 biogenesis.
  • Synthesis of information on ABCG2 structure, function, and implications in cancer.

Main Results:

  • Small molecule compounds can modulate ABCG2 biogenesis by accelerating its endocytosis and lysosomal degradation.
  • This modulation effectively reduces the half-life of ABCG2.
  • Targeting ABCG2 stability presents a potential therapeutic approach.

Conclusions:

  • Modulating ABCG2 stability by targeting its biogenesis is a promising strategy for overcoming MDR in human cancers.
  • Reducing ABCG2 levels could sensitize drug-resistant cancers, offering new therapeutic avenues.
  • Further research into ABCG2 structure, function, and modulation is crucial for developing effective cancer therapies.
Keywords:
ATP-binding cassetteHuman ABCG2cancerchemotherapyfunctionmultidrug resistancestructure

More Related Videos

ABCG5/G8 Crystallization in a Lipidic Bicelle Environment for X-Ray Crystallography06:47

ABCG5/G8 Crystallization in a Lipidic Bicelle Environment for X-Ray Crystallography

Published on: August 25, 2023

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...
Membrane Transporters01:31

Membrane Transporters

Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
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...
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...