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首页> 外文期刊>Expert opinion on therapeutic targets >HIV-1 entry inhibitors: closing the front door.
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HIV-1 entry inhibitors: closing the front door.

机译：HIV-1进入抑制剂：关闭前门。

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摘要

Highly active antiretroviral therapy (HAART) has led to major declines in morbidity and mortality of HIV-1-infected individuals, but the increasing prevalence of drug-resistant viral isolates, combined with the toxicity and other limitations of current treatments, make the development of new therapies a high priority. As knowledge of viral entry has expanded, this step of the viral life cycle has become a target for novel therapeutic strategies. An emerging group of antiretrovirals, known collectively as entry inhibitors, targets several distinct steps in viral entry including CD4 binding, chemokine receptor engagement and the structural changes in the viral envelope required for fusion between viral and cellular membranes. Many entry inhibitors are in various stages of clinical development, with one already licensed for use. This review will provide an overview of the mechanisms involved in the entry process, highlight promising entry blockers under development and discuss several considerations related to treatment that are unique to this class of antiretroviral drugs.
机译：高效的抗逆转录病毒疗法（HAART）导致HIV-1感染者的发病率和死亡率大幅下降，但是耐药病毒分离株的患病率增加，加上当前治疗方法的毒性和其他局限性，导致了这种疾病的发展。新疗法是当务之急。随着病毒进入的知识的扩展，病毒生命周期的这一步骤已成为新型治疗策略的目标。新兴的一组抗逆转录病毒药（统称为进入抑制剂）以病毒进入的几个不同步骤为目标，这些步骤包括CD4结合，趋化因子受体参与和病毒膜与细胞膜融合所需的病毒包膜结构变化。许多进入抑制剂处于临床开发的各个阶段，其中一种已经获得许可使用。这篇综述将概述进入过程中涉及的机制，重点介绍正在开发的有希望的进入阻断剂，并讨论与此类抗逆转录病毒药物独特的治疗相关的几个注意事项。

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