Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy.
CNR-NANOTEC, Licryl-UOS Cosenza and CEMIF.Cal, Department of Physics, University of Calabria, Via P. Bucci, 87036 Rende (CS), Italy.
Molecules. 2019 Feb 2;24(3):550. doi: 10.3390/molecules24030550.
HIV entry in the host cell requires the interaction with the CD4 membrane receptor, and depends on the activation of one or both co-receptors CCR5 and CXCR4. Former selective co-receptor antagonists, acting at early stages of infection, are able to impair the receptor functions, preventing the viral spread toward AIDS. Due to the capability of HIV to develop resistance by switching from CCR5 to CXCR4, dual co-receptor antagonists could represent the next generation of AIDS prophylaxis drugs. We herein present a survey on relevant results published in the last few years on compounds acting simultaneously on both co-receptors, potentially useful as preventing agents or in combination with classical anti-retroviral drugs based therapy.
HIV 进入宿主细胞需要与 CD4 膜受体相互作用，并依赖于一个或两个共受体 CCR5 和 CXCR4 的激活。以前的选择性共受体拮抗剂，在感染的早期阶段发挥作用，能够损害受体功能，阻止病毒向艾滋病的传播。由于 HIV 通过从 CCR5 切换到 CXCR4 来产生耐药性的能力，双重共受体拮抗剂可能代表下一代艾滋病预防药物。本文综述了近年来发表的关于同时作用于两种共受体的化合物的相关研究结果，这些化合物可能具有预防作用，或与基于经典抗逆转录病毒药物的联合治疗相结合。
