The blood-brain barrier is the capillary endothelium between blood and brain that controls what goes in and comes out of the central nervous system (CNS). one major factor contributing to barrier function is a group of ATP-binding cassette (ABC) drug efflux transporters that restrict brain uptake of xenobiotics including a large number of CNS therapeutics. recent research has focused on the regulation of these transporters with the goal of finding the molecular switches to selectively modulate transporter expression and function for improving brain drug delivery. The findings of this research are summarized in this short review.
