Entry inhibitors and their use in the treatment of HIV-1 infection

被引：114

作者：

Haqqani, Aiman A. ^{[1
]}

Tilton, John C. ^{[1
]}

机构：

[1] Case Western Reserve Univ, Case Ctr Prote & Bioinformat, Cleveland, OH 44106 USA

来源：

ANTIVIRAL RESEARCH | 2013年 / 98卷 / 02期

关键词：

HIV; Antiretroviral; Drug; Entry; Inhibitors; Treatment; HUMAN-IMMUNODEFICIENCY-VIRUS; TREATMENT-EXPERIENCED PATIENTS; ENVELOPE GLYCOPROTEIN TRIMERS; TREATMENT-NAIVE PATIENTS; ENFUVIRTIDE RESISTANCE MUTATIONS; SYNCYTIUM-INDUCING PHENOTYPE; ANTI-CD4; MONOCLONAL-ANTIBODY; CLINICAL ISOLATES RESISTANT; CXCR4 RECEPTOR INHIBITOR; SMALL-MOLECULE;

D O I：

10.1016/j.antiviral.2013.03.017

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

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. (C) 2013 Elsevier B.V. All rights reserved.

引用

页码：158 / 170

页数：13

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