Amity Institute of Biotechnology, Amity University, Mumbai, Maharashtra, 410206, India.
Regenerative Medicine Laboratory, Department of Zoology, School of Life Sciences, Periyar University, Salem, Tamil Nadu, 636011, India.
Arch Microbiol. 2023 Mar 26;205(4):142. doi: 10.1007/s00203-023-03461-8.
AIDS (Acquired immunodeficiency syndrome) is one of the chronic and potentially life-threatening epidemics across the world. Hitherto, the non-existence of definitive drugs that could completely cure the Human immunodeficiency virus (HIV) implies an urgent necessity for the discovery of novel anti-HIV agents. Since integration is the most crucial stage in retroviral replication, hindering it can inhibit overall viral transmission. The 5 FDA-approved integrase inhibitors were computationally investigated, especially owing to the rising multiple mutations against their susceptibility. This comparative study will open new possibilities to guide the rational design of novel lead compounds for antiretroviral therapies (ARTs), more specifically the structure-based design of novel Integrase strand transfer inhibitors (INSTIs) that may possess a better resistance profile than present drugs. Further, we have discussed potent anti-HIV natural compounds and their interactions as an alternative approach, recommending the urgent need to tap into the rich vein of indigenous knowledge for reverse pharmacology. Moreover, herein, we discuss existing evidence that might change in the near future.
艾滋病（获得性免疫缺陷综合征）是世界范围内一种慢性且潜在威胁生命的传染病。迄今为止，尚无能够完全治愈人类免疫缺陷病毒（HIV）的特效药物，因此迫切需要发现新型抗 HIV 药物。由于整合是逆转录病毒复制过程中最关键的阶段，抑制整合可以阻止病毒的整体传播。本文对 5 种已获得 FDA 批准的整合酶抑制剂进行了计算研究，特别是由于其耐药性不断增加，需要进行研究。本研究将为抗逆转录病毒治疗（ART）的新型先导化合物的合理设计提供新的可能性，特别是新型整合酶链转移抑制剂（INSTIs）的基于结构的设计，其可能具有比现有药物更好的耐药性特征。此外，我们还讨论了作为替代方法的具有强大抗 HIV 作用的天然化合物及其相互作用，建议迫切需要利用本土知识的丰富资源进行反向药理学研究。此外，本文还讨论了可能在不久的将来发生变化的现有证据。
