title: Role of CNS transporters in the pharmacotherapy of HIV-1 associated neurological disorders.
abstract: Membrane-associated drug transporters are important determinants of antiretroviral drug disposition in the central nervous system during HIV-1 infection. A number of influx and efflux transport proteins expressed at the blood-brain barrier, blood-cerebrospinal fluid barrier and in brain parenchyma cellular compartments (i.e., astrocytes, microglia) have been implicated in the traffic of many antiretroviral drugs into and out of the brain. In particular, members of the ATP-binding cassette membrane associated transporter superfamily and Solute Carrier family are known to be involved in the efflux and/or influx of drugs, respectively. As a result, changes in the functional expression of these transporters can alter the disposition and distribution of drugs in the brain. Moreover, antiretroviral therapy itself and/or pathological events (i.e., inflammation, oxidative stress) associated with viral infection may affect the functional expression of these transporters. This review summarizes recent knowledge on the role of drug transporters in regulating brain antiretroviral drug transport in the context of HIV-1 infection.
authors.forename: Tamima
authors.initials: T
authors.lastname: Ashraf
authors.forename: Kevin
authors.initials: K
authors.lastname: Robillard
authors.forename: Gary N Y
authors.initials: GN
authors.lastname: Chan
authors.affiliation: Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, 144 College Street, Room 1001, Toronto, ON, Canada, M5S 3M2. r.bendayan@utoronto.ca.
authors.forename: Reina
authors.initials: R
authors.lastname: Bendayan
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000627:therapeutic use*; D001812:Blood-Brain Barrier / Q000187:drug effects / Q000378:metabolism*; D016503:Drug Delivery Systems; D015658:HIV Infections / Q000150:complications / Q000188:drug therapy / Q000821:virology*; D015497:HIV-1; D006801:Humans; D026901:Membrane Transport Proteins / Q000378:metabolism*; D009422:Nervous System Diseases / Q000188:drug therapy* / Q000209:etiology / Q000378:metabolism*
chemical_list: D019380:Anti-HIV Agents; D026901:Membrane Transport Proteins