title: Entry inhibitors and their use in the treatment of HIV-1 infection.
abstract: Entry of HIV into target cells is a complex, multi-stage process involving sequential attachment and CD4 binding, coreceptor binding, and membrane fusion. HIV entry inhibitors are a complex group of drugs with multiple mechanisms of action depending on the stage of the viral entry process they target. Two entry inhibitors are currently approved for the treatment of HIV-infected patients. Maraviroc, a CCR5 antagonist, blocks interactions between the viral envelope proteins and the CCR5 coreceptor. Enfuvirtide, a fusion inhibitor, disrupts conformational changes in gp41 that drive membrane fusion. A wide array of additional agents are in various stages of development. This review covers the entry inhibitors and their use in the treatment of HIV-infected patients.
authors.affiliation: Case Center for Proteomics and Bioinformatics, Case Western Reserve University, Cleveland, OH 44106, USA.
authors.forename: Aiman A
authors.initials: AA
authors.lastname: Haqqani
authors.forename: John C
authors.initials: JC
authors.lastname: Tilton
mesh_terms: D000818:Animals; D024882:Drug Resistance, Viral; D023581:HIV Fusion Inhibitors / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D053586:Virus Internalization / Q000187:drug effects
chemical_list: D023581:HIV Fusion Inhibitors