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Updated: Nov 21, 2025

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors
Chao Zhang1, Qian Xie1, Chi Cheong Wan2
1Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang110016, China.
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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