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SARS-CoV-2 Entry Inhibitors Targeting Virus-ACE2 or Virus-TM-PRSS2 Interactions

Journal

CURRENT MEDICINAL CHEMISTRY
Volume 29, Issue 4, Pages 682-699

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867328666210420103021

Keywords

SARS-CoV-2; COVID-19; spike protein; angiotensin-converting enzyme 2; transmembrane protease; serine 2; drug design

Funding

  1. Shandong Provincial Key research and development project [2019JZZY021011]
  2. National Science and Technology Major Projects for Major New Drugs Inno-vation and Development [2019ZX09301126]
  3. Science Foundation for Outstanding Young Scholars of Shan-dong Province [ZR2020JQ31]
  4. Science Foundation for Excellent Young Scholars of Shandong Province [ZR2020YQ61]
  5. Foreign cultural and educational ex-perts Project [GXL20200015001]
  6. Qilu Young Scho-lars Program of Shandong University
  7. Taishan Scholar Program at Shandong Province

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This article provides concise information on potential entry inhibitors targeting the virus-ACE2 or virus-TMPRSS2 interactions in SARS-CoV-2, which can effectively prevent virus infection.
COVID-19 is an infectious disease caused by SARS-CoV-2. The life cycle of SARS-CoV-2 includes the entry into the target cells, replicase translation, replicating and transcribing genomes, translating structural proteins, assembling and releasing new virions. Entering host cells is a crucial stage in the early life cycle of the virus, and blocking this stage can effectively prevent virus infection. SARS enters the target cells mediated by the interaction between the viral S protein and the target cell surface receptor angiotensin-converting enzyme 2 (ACE2), as well as the cleavage effect of a type-II transmembrane serine protease (TMPRSS2) on the S protein. Therefore, the ACE2 receptor and TMPRSS2 are important targets for SARS-CoV-2 entry inhibitors. Herein, we provide a concise report/information on drugs with potential therapeutic value targeting virus-ACE2 or virus-TMPRSS2 interactions to provide a reference for the design and discovery of potential entry inhibitors against SARS-CoV-2.

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