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Review
. 2014;20(10):1450-62.
doi: 10.2174/13816128113199990466.

Human ABC transporters at blood-CNS interfaces as determinants of CNS drug penetration

Catarina Chaves  1   2   3 , Ramzi Shawahna  1   2   4 , Aude Jacob  1   2 , Jean-Michel Scherrmann  1   2 , Xavier Declèves  1   2
Affiliations
Review

Human ABC transporters at blood-CNS interfaces as determinants of CNS drug penetration

Catarina Chaves et al. Curr Pharm Des. 2014.

Abstract

Since the discovery of P-glycoprotein (P-gp) in brain microvessels composing the human blood-brain barrier (BBB), ATP-binding cassette (ABC) transporters have been recognized as bottlenecks in the development and delivery of neuropharmaceuticals. ABC transporters are expressed predominately at the plasma luminal membrane of brain capillary endothelial cells. These ABC transporters are responsible for the efflux of their substrates from the endothelial cells to the bloodstream against the concentration gradient and thus limit the entry of some drugs within the central nervous system (CNS). Advanced quantitative molecular biology tools allowed gene and protein quantification of the components of microvessels isolated from different species including human. Recently, positron emission tomography using radiolabelled probes that are substrates of ABC transporters allowed the determination of their functional activity at the human BBB. Here, we summarized new information regarding the relative expression, substrate recognition pattern for CNS drugs and functional activity of ABC transporters that are quantitatively expressed at the human BBB.

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