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Screening and evaluation of small molecule activators for premature activation of HIV-1 precursors
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Ling MA1, Jia-jia WEN1, Xiao-yu LI1, Tao WEI2, *, Shan CEN1, *
Acta Pharmaceutica Sinica | 2021, 56(6) : 1627 - 1633
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Acta Pharmaceutica Sinica | 2021, 56(6): 1627-1633
• Original Articles •
Screening and evaluation of small molecule activators for premature activation of HIV-1 precursors
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Ling MA1, Jia-jia WEN1, Xiao-yu LI1, Tao WEI2, *, Shan CEN1, *
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2. College of Applied Arts and Science of Beijing Union University, Beijing 100191, China
Published: 2021-06-12 doi: 10.16438/j.0513-4870.2021-0311
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Strict regulation of human immunodeficiency virus type 1 (HIV-1) protease function is critical for efficient production of mature viral particles. During viral protein expression and viral assembly, HIV-1 protease (PR) located within Gag-Pol precursor must be inactive to prevent premature cytoplasmic processing of the viral Gag and Gag-Pol precursors. Premature activation of HIV-1 precursors leads to major defects in viral assembly and production of viral particles. Specifically activating the protease in the precursor protein can directly inhibit the replication of the virus. In addition, HIV-1 PR is able to induce cell apoptosis. In this study, we identified 6 small molecule compounds using a cell-based assay for screening compounds that activate HIV-1 PR and induce premature of HIV-1 precursors. Results showed the active compounds are able to activate HIV-1 PR, inhibit HIV-1 replication, and induce cell apoptosis. This study provides ideas for the research and development of antiviral drugs.

anti-HIV-1 drug  /  screening assay  /  protease  /  precursor  /  premature
Ling MA, Jia-jia WEN, Xiao-yu LI, Tao WEI, Shan CEN. Screening and evaluation of small molecule activators for premature activation of HIV-1 precursors[J]. Acta Pharmaceutica Sinica, 2021 , 56 (6) : 1627 -1633 . DOI: 10.16438/j.0513-4870.2021-0311
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Article Info
doi: 10.16438/j.0513-4870.2021-0311
  • Receive Date：2021-03-05
  • Online Date：2025-12-18
  • Published：2021-06-12
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History
  • Received：2021-03-05
  • Revised：2021-04-06
Funding
Affiliations
    1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2. College of Applied Arts and Science of Beijing Union University, Beijing 100191, China
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