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Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors

[ Vol. 28 , Issue. 24 ]

Author(s):

Chao Zhang, Qian Xie, Chi Cheong Wan, Zhe Jin* and Chun Hu*   Pages 4910 - 4934 ( 25 )

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.

Affiliation:

Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016, Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016, School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong SAR, Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016, Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016



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