Role and modulation of drug transporters in HIV-1 therapy

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• 作者：Camille Alam ; Sana-Kay Whyte-Allman ; Amila Omeragic ; Reina Bendayan ; ^{r.bendayan@utoronto.ca" class="auth_mail" title="E-mail the corresponding author}
• 关键词：ABC transporter ; ATP-binding cassette membrane transporter ; AhR ; Aryl hydrocarbon receptor ; AIDS ; Acquired immunodeficiency syndrome ; ARV ; Antiretroviral drug ; BBB ; Blood&ndash ; brain barrier ; BCRP ; Breast cancer resistance protein ; BTB ; Blood&ndash ; testicular barrier ; CAR ; Constitutive androstane receptor ; CCR5 ; Cysteine&ndash ; cysteine receptor 5 ; CD4 ; Cluster of differentiation-4 ; CNS ; Central nervous system ; CNT ; Concentrative nucleoside transporter ; CPE ; CNS penetration effectiveness ; CVF ; Ce
• 刊名：Advanced Drug Delivery Reviews
• 出版年：2016
• 出版时间：1 August 2016
• 年：2016
• 卷：103
• 期：Complete
• 页码：121-143
• 全文大小：1146 K

文摘

Current treatment of human immunodeficiency virus type-1 (HIV-1) infection involves a combination of antiretroviral drugs (ARVs) that target different stages of the HIV-1 life cycle. This strategy is commonly referred to as highly active antiretroviral therapy (HAART) or combined antiretroviral therapy (cART). Membrane-associated drug transporters expressed ubiquitously in mammalian systems play a crucial role in modulating ARV disposition during HIV-1 infection. Members of the ATP-binding cassette (ABC) and solute carrier (SLC) transporter superfamilies have been shown to interact with ARVs, including those that are used as part of first-line treatment regimens. As a result, the functional expression of drug transporters can influence the distribution of ARVs at specific sites of infection. In addition, pathological factors related to HIV-1 infection and/or ARV therapy itself can alter transporter expression and activity, thus further contributing to changes in ARV disposition and the effectiveness of HAART. This review summarizes current knowledge on the role of drug transporters in regulating ARV transport in the context of HIV-1 infection.