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高活性逆转录治疗方法抗病毒作用强,为欧美发达国家治疗艾滋病的常规方法。然而,这种方法并不能清除整合在CD4+T淋巴细胞中的HIV-1的DNA,对中晚期感染者效果不明显,长期服用产生耐药性、毒副作用以及费用昂贵,使其治疗艾滋病越来越受到限制。属于G蛋白偶联受体家族趋化因子受体5(CCR5)的发现为开发新型抗病毒药物找到了方向。CCR5是HIV-1进入巨噬细胞过程中发挥重要作用的一个辅助受体,是抗艾滋病药物作用的重要靶点之一。目前,已有许多活性强、选择性高的小分子CCR5拮抗剂进入了临床试验阶段。本文对近年来文献报道的小分子CCR5拮抗剂进行综述。
High activity of reverse transcription treatment of anti-virus effect is strong, for developed countries in Europe and America AIDS treatment of conventional methods. However, this method does not clear the DNA of HIV-1 that is integrated in CD4 + T lymphocytes. It is not effective in patients with advanced or middle-stage infections. Drug resistance, toxicity and side effects and long-term use are expensive and expensive. The more limited. The discovery of chemokine receptor 5 (CCR5), a member of the G-protein coupled receptor family, has found a way to develop novel antiviral drugs. CCR5 is a co-receptor that plays an important role in HIV-1 entry into macrophages and is one of the important targets of anti-AIDS drugs. At present, many active and selective small molecule CCR5 antagonists have entered the clinical trial phase. This review summarizes small molecule CCR5 antagonists reported in the literature in recent years.