摘要
HIV-1整合酶在反转录过程中催化病毒DNA插入人类细胞基因组。由于整合酶在人类细胞中缺乏同源物以及它在HIV-1复制中的重要作用,整合酶是一个有吸引力的治疗靶点。尽管HIV-1整合酶抑制剂的研究取得了重大进展,但一些棘手的问题,如耐药性,阻碍了HIV-1整合酶抑制剂的进一步研究。本文简要介绍了HIV-1整合酶的结构、功能和催化机制,并对近年来HIV-1整合酶小分子抑制剂的研究进展作出了不同的结论。
关键词: 艾滋病,整合酶,HIV-1整合酶抑制剂,抗艾滋病药物,双抑制剂,变构整合酶抑制剂。
Current Medicinal Chemistry
Title:Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors
Volume: 28 Issue: 24
关键词: 艾滋病,整合酶,HIV-1整合酶抑制剂,抗艾滋病药物,双抑制剂,变构整合酶抑制剂。
摘要: 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.
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Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors, Current Medicinal Chemistry 2021; 28 (24) . https://dx.doi.org/10.2174/0929867328666210114124744
DOI https://dx.doi.org/10.2174/0929867328666210114124744 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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