ABC Transporters at the Blood–Brain Barrier

  • David S. Miller
Part of the Topics in Medicinal Chemistry book series (TMC, volume 10)


In the blood–brain barrier several ABC transporters are expressed at the luminal, blood-facing, plasma membrane of the brain capillary endothelial cells. There they function as ATP-driven efflux pumps for xenobiotics and endogenous metabolites, thus providing an important element of the barrier. When these transporters limit neurotoxicant entry into the CNS, they are neuroprotective; when they limit therapeutic drug entry, they become major obstacles to drug delivery to treat CNS diseases. Here I review function and regulation of ABC transporters at the blood–brain barrier, with an emphasis on recently disclosed mechanisms that alter transporter expression and transport activity.


BCRP Blood–brain barrier Brain capillary endothelium Disease Drug delivery MRP P-glycoprotein Regulation 



ATP-binding cassette


Alzheimer’s disease


Antiepileptic drugs


Arylhydrocarbon receptor


Protein kinase B


Apolipoprotein E


Breast cancer resistance protein (ABCG2)


Bile salt export pump


Constitutive androstane receptor


Cystic fibrosis transmembrane regulator (ABCC7)


Central nervous system






Prostaglandin E2 receptor


Estrogen receptor


Farnesyl-X receptor


Glycogen synthase kinase 3 beta


Human amyloid precursor protein


Inducible nitric oxide synthase


c-Jun N-terminal kinase


Liver-X receptor


Multidrug resistance-associated protein


Nuclear factor kappa-light-chain-enhancer of activated B cells




Polychlorinated biphenyls




Polymerase chain reaction


Phosphatidylinositide 3-kinase




Protein kinase C isoform β1


Phosphatase and tensin homolog


Pregnane-X receptor




Sphingosine-1-phosphate receptor 1


Tumor necrosis factor-α


Vitamin D receptor


Vascular endothelial growth factor



This work was supported by the Intramural Research Program of the National Institute of Environmental Health Sciences, National Institutes of Health. I thank all the past and present members of my laboratory for their hard work and creativity.


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Copyright information

© Springer-Verlag Berlin Heidelberg 2013

Authors and Affiliations

  • David S. Miller
    • 1
  1. 1.Laboratory of Toxicology and PharmacologyNIH/NIEHSResearch Triangle ParkUSA

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