ISF College of Pharmacy, Moga-142001, Punjab, India.
Department of Chemistry, Maharishi Markandeshwar (Deemed to be University), Mullana-133207, Haryana, India.
Curr Top Med Chem. 2018;18(31):2664-2680. doi: 10.2174/1568026619666190119143239.
HIV-1 integrase, a member of a polynucleotidyl transferases superfamily, catalyzes the insertion of the viral DNA into the genome of host cells. It has emerged as a potential target for developing anti-HIV agents. In the last two decades, a number of integrase inhibitors have been developed as potential anti-HIV therapeutics. Several integrase inhibitors have reached later stages of clinical trials including S-1360, L870,810, L870,812 and BMS-707035. Into the bargain, Raltegravir, Elvitegravir and Dolutegravir have been approved by FDA as anti-HIV agents. This review article summarizes the structural insights required for the inhibition of the HIV1 integrase in the context of clinically relevant HIV1 integrase inhibitors. Additionally, the structural features required for overcoming HIV resistance have been discussed. These insights will update the ongoing design of novel antiviral inhibitors.
HIV-1 整合酶属于多核苷酸转移酶超家族成员，可催化病毒 DNA 插入宿主细胞基因组。它已成为开发抗 HIV 药物的潜在靶标。在过去的二十年中，已经开发了许多整合酶抑制剂作为潜在的抗 HIV 治疗药物。几种整合酶抑制剂已进入临床试验的后期阶段，包括 S-1360、L870810、L870812 和 BMS-707035。此外，拉替拉韦、艾维雷格韦和多替拉韦已被 FDA 批准为抗 HIV 药物。本文综述了与临床相关的 HIV1 整合酶抑制剂相关的 HIV1 整合酶抑制所需的结构见解。此外，还讨论了克服 HIV 耐药性所需的结构特征。这些见解将更新正在进行的新型抗病毒抑制剂的设计。
