Abstract
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.
Keywords: AIDS, integrase, HIV-1 integrase inhibitors, anti-AIDS drugs, dual inhibitors, allosteric integrase inhibitors.
Current Medicinal Chemistry
Title:Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors
Volume: 28 Issue: 24
Author(s): Chao Zhang, Qian Xie, Chi Cheong Wan, Zhe Jin*Chun Hu*
Affiliation:
- Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016,China
- Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016,China
Keywords: AIDS, integrase, HIV-1 integrase inhibitors, anti-AIDS drugs, dual inhibitors, allosteric integrase inhibitors.
Abstract: 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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Cite this article as:
Zhang Chao , Xie Qian , Wan Cheong Chi , Jin Zhe *, Hu Chun *, 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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