Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016, China.
School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong SAR, China.
Curr Med Chem. 2021;28(24):4910-4934. doi: 10.2174/0929867328666210114124744.
HIV-1 integrase catalyzed the insertion of viral DNA into the genome of human cells in the process of retrotranscription. Integrase is an attractive target for HIV-1 treatment due to the lack of its homologue in human cells and its vital role in HIV-1 replication. Although major progress in the development of HIV-1 integrase inhibitors has been made, some thorny problems, such as drug resistance, led to the further study of HIV-1 integrase inhibitors. This review briefly discussed the structure, function, and mechanism of catalysis of HIV-1 integrase and made a different conclusion for recent advances in small-molecule inhibitors of HIV-1 integrase.
HIV-1 整合酶在逆转录过程中催化病毒 DNA 插入人类细胞的基因组。由于其在人类细胞中没有同源物，并且在 HIV-1 复制中起着至关重要的作用，整合酶是 HIV-1 治疗的一个有吸引力的靶点。尽管在开发 HIV-1 整合酶抑制剂方面取得了重大进展，但一些棘手的问题，如耐药性，导致了对 HIV-1 整合酶抑制剂的进一步研究。本文简要讨论了 HIV-1 整合酶的结构、功能和催化机制，并对 HIV-1 整合酶小分子抑制剂的最新进展得出了不同的结论。
