title: Drug transport to the brain: key roles for the efflux pump P-glycoprotein in the blood-brain barrier.
abstract: 1. The blood-brain barrier (BBB) contributes to brain homeostastis and fulfills a protective function by controlling the access of solutes and toxic substances to the central nervous system (CNS). The efflux transporter P-glycoprotein (P-gp) is a key element of the molecular machinery that confers special permeability properties to the BBB. 2. P-gp, which was initially recognized for its ability to expel anticancer drugs from multidrug-resistant cancer cells, is strongly expressed in brain capillaries. Its expression in the BBB limits the accumulation of many hydrophobic molecules and potentially toxic substances in the brain. 3. The purpose of this review is to summarize the current state of knowledge about the expression of P-gp, its cellular localization as well as its possible functions in the BBB.
authors.affiliation: Laboratoire de Médecine Moléculaire, Hôpital Sainte-Justine-Université du Québec à Montréal, C.P. 8888, Succursale Centre-ville, Montréal, Quebec, Canada H3C 3P8.
authors.forename: Michel
authors.initials: M
authors.lastname: Demeule
authors.forename: Anthony
authors.initials: A
authors.lastname: Régina
authors.forename: Julie
authors.initials: J
authors.lastname: Jodoin
authors.forename: Alain
authors.initials: A
authors.lastname: Laplante
authors.forename: Claude
authors.initials: C
authors.lastname: Dagenais
authors.forename: France
authors.initials: F
authors.lastname: Berthelet
authors.forename: Albert
authors.initials: A
authors.lastname: Moghrabi
authors.forename: Richard
authors.initials: R
authors.lastname: Béliveau
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000970:Antineoplastic Agents / Q000378:metabolism / Q000494:pharmacology; D001692:Biological Transport; D001812:Blood-Brain Barrier; D001921:Brain / Q000098:blood supply / Q000378:metabolism; D001932:Brain Neoplasms / Q000378:metabolism; D002986:Clinical Trials as Topic; D019008:Drug Resistance, Neoplasm; D004730:Endothelium, Vascular / Q000166:cytology / Q000378:metabolism; D006801:Humans; D008833:Microcirculation / Q000166:cytology / Q000378:metabolism
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents