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Related Concept Videos

Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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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...
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ABC Transporters: Exporter01:31

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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...
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ABC Transporters: Importer01:27

ABC Transporters: Importer

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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:
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Transcytosis of IgG01:15

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Transcytosis is the process in which molecules are internalized by endocytosis, transported across the cell, and released through exocytosis from the opposite end of the cell. Molecules such as insulin, immunoglobulins, and certain nutrients are transferred through the recycling endosomes by recycling and transcytosis.
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Transcellular Transport of Solutes01:23

Transcellular Transport of Solutes

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Transcellular transport of solutes is the movement of substances like monosaccharides and amino acids through polarized cells. This transport mechanism is primarily seen in epithelial and endothelial cells aided by membrane transport proteins such as channels and transporters. The tight junctions between these cells confine the membrane proteins to the two sides of the cell. The epithelial cells have distinct apical and basolateral domains. In contrast, the endothelial cells show the luminal...
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Glucose Absorption Into the Small Intestine01:26

Glucose Absorption Into the Small Intestine

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Complex carbohydrates consumed cannot be absorbed into the small intestine in their original form. First, they must be hydrolyzed to a monosaccharide form such as glucose or galactose. These monosaccharides are then transported across the intestinal membrane and into the blood via transcellular transport. The intestinal epithelial cells allow the movement of these monosaccharides with a defined 'entry' through membrane transporter proteins present on their apical membrane and...
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An Intravital Microscopy-Based Approach to Assess Intestinal Permeability and Epithelial Cell Shedding Performance
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Expression, Function, and Regulation of ABCG2 on the Intestinal Epithelial Barrier Permeability.

Ping Shi1, Lianhua Tang1, Fei Yin1,2

  • 1College of Pharmacy and Bioengineering, Chongqing University of Technology, Chongqing, 400054, People's Republic of China.

Current Drug Metabolism
|April 15, 2025
PubMed
Summary

Human breast cancer resistance protein (BCRP, ABCG2) in the intestine limits xenobiotic absorption and influences drug response. Its function is key to intestinal barrier integrity and drug disposition.

Keywords:
ATP-binding cassette (ABC) efflux transporter 2 (ABCG2)drug transportgene symbolintestinal barrier dysfunctionintestinal epithelial permeabilitysystemic circulation.

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Area of Science:

  • Pharmacology
  • Gastroenterology
  • Molecular Biology

Background:

  • Human breast cancer resistance protein (BCRP, ABCG2) is an ATP-binding cassette efflux transporter highly expressed in the intestinal epithelium.
  • The intestinal epithelial monolayer serves as a critical barrier between the body and the external environment.
  • Intestinal ABCG2 significantly impacts the absorption, distribution, and elimination of xenobiotics and endogenous molecules.

Purpose of the Study:

  • To review the role of intestinal ABCG2 in drug transport.
  • To summarize ABCG2's involvement in intestinal urate excretion.
  • To discuss ABCG2's contribution to intestinal barrier dysfunction and permeability changes in human intestinal disorders.

Main Methods:

  • Literature review of existing research on ABCG2 in the intestinal epithelium.
  • Analysis of studies investigating ABCG2's role in xenobiotic absorption and drug disposition.
  • Examination of research on ABCG2's impact on intestinal barrier function and disease.

Main Results:

  • Intestinal ABCG2 limits the absorption of its substrates in the small intestine.
  • Changes in ABCG2 expression and activity affect drug response and side effects.
  • ABCG2 plays a role in intestinal urate excretion and barrier dysfunction.

Conclusions:

  • Intestinal ABCG2 is a critical determinant of drug absorption and disposition.
  • ABCG2 function influences intestinal barrier integrity and permeability.
  • Dysregulation of intestinal ABCG2 is implicated in various human intestinal disorders and impacts therapeutic outcomes.