Department of Molecular Biology and Microbiology and Division of Infectious Diseases, Department of Medicine, Case Western Reserve University, 10900 Euclid Ave., Cleveland, OH 44106, USA.
Viruses. 2010 May;2(5):1069-1105. doi: 10.3390/v2051069. Epub 2010 Apr 29.
Entry inhibitors represent a new class of antiretroviral agents for the treatment of infection with HIV-1. While resistance to other HIV drug classes has been well described, resistance to this new class is still ill defined despite considerable clinical use. Several potential mechanisms have been proposed: tropism switching (utilization of CXCR4 instead of CCR5 for entry), increased affinity for the coreceptor, increased rate of virus entry into host cells, and utilization of inhibitor-bound receptor for entry. In this review we will address the development of attachment, fusion, and coreceptor entry inhibitors and explore recent studies describing potential mechanisms of resistance.
进入抑制剂是一类新的抗逆转录病毒药物，用于治疗感染 HIV-1。虽然其他 HIV 药物类别的耐药性已经得到了很好的描述，但尽管已经有了大量的临床应用，这种新的药物类别的耐药性仍然没有得到很好的定义。已经提出了几种潜在的机制：趋性转换（利用 CXCR4 而不是 CCR5 进入）、增加与共受体的亲和力、增加病毒进入宿主细胞的速度，以及利用抑制剂结合的受体进入。在这篇综述中，我们将讨论附着、融合和共受体进入抑制剂的发展，并探讨描述潜在耐药机制的最新研究。
