埃替拉韦
整合酶
雷特格韦
杜鲁特格拉维尔
整合酶抑制剂
背景(考古学)
人类免疫缺陷病毒(HIV)
计算生物学
病毒学
抗逆转录病毒药物
药品
生物
药理学
抗逆转录病毒疗法
病毒载量
古生物学
作者
Maninder Kaur,Ravindra K. Rawal,Goutam Rath,Amit K. Goyal
标识
DOI:10.2174/1568026619666190119143239
摘要
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.
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