Data for: Effect of amyloid beta on ATP-Binding Cassette transporter expression and activity in porcine brain microvascular endothelial cells

The blood-brain barrier (BBB) is highly restrictive in nature and helps maintain the privileged
site status of the central nervous system (CNS). ATP-binding Cassette (ABC) transporters are
major functional components of the BBB and significantly influence the BBB permeation of
both endogenous and exogenous compounds.
One of the key pathological characteristics of Alzheimer’s disease is production and
aggregation of the amyloid beta (Aβ(1-42)) peptide within the brain. Whilst it has been
demonstrated Aβ(1-42) reduces expression and activity of the ABCB1 efflux transporter in brain
endothelial cells, no studies yet report the effects of Aβ(1-42) on the activity, or expression, of
ABCC5 and ABCG2, which are other key efflux transporters expressed in the BBB.
The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are widely
expressed in BBB brain endothelial cells and are key regulators of ABC transporter expression.
However, to date, no studies report the effects of Aβ(1-42) on PXR and CAR expression.
The present study is the first to demonstrate that Aβ(1-42) is able to modify the expression and
activity of multiple ABC efflux transporters, as well as modify expression of nuclear receptors
which regulate transporter expression. These findings suggest that interaction of Aβ(1-42) with
BBB endothelial cells down-regulates protective mechanisms within the BBB and may impact
on penetration of compounds across the BBB.