Affiliation:
1. State Key Laboratory of Natural Medicines, School of Basic Medical Sciences and Clinical Pharmacy, China Pharmaceutical University, Nanjing 210009, China
2. Department of Surgery, Stanford University School of Medicine, Stanford, CA 94305, United States
Abstract
P-glycoprotein (P-gp) is a member of ATP-Binding Cassette (ABC) transporter family. Because
of its characteristic luminal surface location, high transport potency and structural specificity, Pgp
is regarded as a selective gatekeeper of the Blood Brain Barrier (BBB) to prevent the entry of toxins
or unwanted substances into the brain. In recent years, increasing evidence has shown that P-gp is
involved in the immune inflammatory response in the Central Nervous System (CNS) disorders by
regulating microglia activation, and mediating immune cell migration. Furthermore, Glucocorticoid
Receptor (GR) may play a crucial role in P-gp-mediated microglia activation and immune cell migration
via GR-mediated mRNA decay. In this article, we will review P-gp structure, distribution, function,
regulatory mechanisms, inhibitors and effects of P-gp in the pathogenesis of several CNS diseases
and will discuss the role of P-gp in microglia activation, immune cell migration and the relationship
with cytokine secretion.
Funder
China Pharmaceutical University
Publisher
Bentham Science Publishers Ltd.
Subject
Clinical Biochemistry,Drug Discovery,Pharmacology,Molecular Medicine
Cited by
14 articles.
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