Division of Infectious Diseases, Weill Medical College of Cornell University, New York, New York 10065, USA.
Annu Rev Med. 2012;63:81-93. doi: 10.1146/annurev-med-052010-145454. Epub 2011 Oct 27.
CCR5 antagonists inhibit HIV-1 entry by blocking the interaction of HIV-1 with the CCR5 cellular receptor. In patients with established HIV-1 infection, some viral strains use an alternative coreceptor for HIV-1 entry, CXCR4; CCR5 antagonists are not effective in patients harboring these viral strains. Coreceptor tropism testing of viral strains in an individual patient is necessary prior to treating with a CCR5 antagonist. There is one CCR5 antagonist, maraviroc, that is FDA-approved for treatment of HIV-1 infection. This drug is used most commonly for the treatment of HIV-1 infection in patients who have failed other antiretroviral regimens. In addition to virologic effects, CCR5 antagonists are under investigation for immune-modulating effects and for HIV-1 prevention. Ongoing research will further elucidate the role of CCR5 antagonists in combating HIV disease.
CCR5 拮抗剂通过阻止 HIV-1 与 CCR5 细胞受体的相互作用来抑制 HIV-1 的进入。在已感染 HIV-1 的患者中,一些病毒株使用 HIV-1 进入的替代共受体 CXCR4;对于携带这些病毒株的患者,CCR5 拮抗剂无效。在使用 CCR5 拮抗剂治疗之前,需要对个体患者的病毒株进行共受体嗜性测试。有一种 CCR5 拮抗剂,马拉维若,被 FDA 批准用于治疗 HIV-1 感染。这种药物最常用于治疗其他抗逆转录病毒方案失败的 HIV-1 感染患者。除了病毒学效果外,CCR5 拮抗剂还在研究其免疫调节作用和 HIV-1 预防作用。正在进行的研究将进一步阐明 CCR5 拮抗剂在对抗 HIV 疾病中的作用。