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image of Expression, Function, and Regulation of ABCG2 on the Intestinal Epithelial Barrier Permeability

  • Expression, Function, and Regulation of ABCG2 on the Intestinal Epithelial Barrier Permeability

  • Authors: Ping Shi, Lianhua Tang, Fei Yin, Hong Guo and Jianhui Liu
  • 1 1College of Pharmacy and Bioengineering, Chongqing University of Technology, Chongqing, 400054, People’s Republic of China ; 2Chongqing  Key  Laboratory  of  Target-Based  Drug  Discovery  and  Research,  Chongqing,  400054,  China ;  3Department  of  Gastroenterology,  Chongqing  General  Hospital, University  of  Chinese  Academy  of  Sciences,  Chongqing,  401147,  People’s Republic of China
  • Source: Current Drug Metabolism
    Available online: 11 April 2025
  • DOI: https://doi.org/10.2174/0113892002368449250331144821
    • Received: 22 Nov 2024
    • Accepted: 04 Feb 2025
    • Available online: 11 Apr 2025

Abstract

Human breast cancer resistance protein (BCRP, gene symbol ABCG2) is an ATP-binding cassette (ABC) efflux transporter that is highly expressed on the apical membranes of intestinal epithelium and contributes to the absorption, distribution, and elimination of xenobiotics and the efflux of endogenous molecules. Also, the intestinal epithelial monolayer is the largest interface and the most important functional barrier between the internal environment and the systemic circulation. Extensive studies have demonstrated that intestinal ABCG2 of humans and rodents plays a crucial role in limiting absorption of xenobiotics, which are ABCG2 transport substrates, in the small intestine by mediating distribution in the intestinal epithelial barrier. Therefore, changes in the expression, function and activity of ABCG2 in the intestinal epithelial barrier play important roles in drug response and side effects. In this review, we specifically summarize the current research progress of ABCG2 in intestinal drug transport, intestinal urate excretion and intestinal barrier dysfunction, and its role in altering the intestinal epithelial barrier permeability in human intestinal disorder.

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/content/journals/cdm/10.2174/0113892002368449250331144821
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Expression, Function, and Regulation of ABCG2 on the Intestinal Epithelial Barrier Permeability
Bentham Science Publishers ; https://doi.org/10.2174/0113892002368449250331144821
/content/journals/cdm/10.2174/0113892002368449250331144821
/content/journals/cdm/10.2174/0113892002368449250331144821
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  • Article Type:     Review Article
Keywords: intestinal epithelial permeability ; drug transport ; intestinal barrier dysfunction ; ATP-binding cassette (ABC) efflux transporter 2 (ABCG2)

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