Induction of P-glycoprotein overexpression in brain endothelial cells as a model to study blood-brain barrier efflux transport

Induction of P-glycoprotein overexpression in brain endothelial cells as a model to study blood-brain barrier efflux transport

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The blood-brain barrier (BBB) is comprised of specialized brain endothelial cells (BECs) that contribute to maintaining central nervous system (CNS) homeostasis.BECs possess properties such as an array of multi-drug efflux transporters that eject various drugs and toxins, preventing their entry into the CNS.Together, it is estimated that these efflux transporters can eject up to 98% of known xenobiotic compounds.

P-glycoprotein (P-gp) is a promiscuous efflux transporter at the BBB and can Cake Set efflux up to 90 various substrates, representing a major hurdle in CNS drug delivery for therapeutic interventions.This necessitates Accessories the study of P-gp to discover drugs that are non-substrates of P-gp as well as to identify novel P-gp inhibitors.Here we report the generation of P-gp overexpressing BECs under the endogenous promoter control that could be used in the screening of P-gp substrates.

These cells could provide utility in the design of drugs or identification of novel inhibitors.