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ABCG2 is not able to catalyze glutathione efflux and does not contribute to GSH-dependent collateral sensitivity

Charlotte Gauthier1, Csilla Ozvegy-Laczka, Gergely Szakacs

  • 1Drug Resistance Mechanism and Modulation Group, Ligue 2013 Certified, Bases Moléculaires et Structurales des Systèmes Infectieux, UMR5086, Centre National de la Recherche Scientifique, Université de Lyon, Institut de Biologie et Chimie des Protéines, University of Lyon Lyon, France.

Frontiers in Pharmacology
|December 7, 2013
PubMed

Insights

This study investigated if the ABCG2 transporter moves glutathione (GSH). Researchers found no evidence that ABCG2 directly transports GSH, unlike the ABCC1 transporter, suggesting a different role in cancer chemoresistance.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • ATP-binding cassette (ABC) transporters play crucial roles in cellular functions, including drug resistance.
  • ABCG2 is a significant transporter involved in cancer cell chemoresistance.
  • ABCC1, another ABC transporter, mediates glutathione (GSH) efflux and can induce collateral sensitivity in multidrug-resistant cells.

Purpose of the Study:

  • To investigate whether ABCG2 mediates active glutathione (GSH) transport.
  • To explore the potential of targeting ABCG2-overexpressing cells through modulation of GSH levels.
  • To determine if ABCG2 interacts directly with GSH.

Main Methods:

  • Assessed the effects of ABCG2 overexpression on intracellular GSH levels in HEK293 and MCF7 cells.
  • Investigated ABCG2-dependent GSH transport using ABCG2 inhibitors and transport modulators.
  • Measured drug-stimulated ATPase activity of ABCG2 in Sf9 insect cell membrane vesicles.
  • Performed direct (3)H-GSH transport assays in membrane vesicles.

Main Results:

  • ABCG2 overexpression altered intracellular GSH levels but did not influence GSH efflux.
  • ABCG2-ATPase activity was not modulated by GSH.
  • Direct transport assays showed that ABCG2 does not catalyze significant GSH transport.
  • No direct interaction between ABCG2 and GSH was detected.

Conclusions:

  • ABCG2 does not appear to directly transport glutathione (GSH).
  • The mechanism of chemoresistance mediated by ABCG2 likely does not involve direct GSH efflux.
  • Further research is needed to understand the long-term modulation of cellular GSH by ABCG2.
Keywords:
breast cancer resistance protein ABCG2collateral sensitivityglutathione effluxintracellular glutathione depletionmodulatorsmultidrug resistance protein ABCC1selective apoptosis

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