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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

SARS-CoV-2 Entry Inhibitors Targeting Virus-ACE2 or Virus-TMPRSS2 Interactions

Author(s): Hao Lin, Srinivasulu Cherukupalli, Da Feng, Shenghua Gao*, Dongwei Kang*, Peng Zhan* and Xinyong Liu*

Volume 29, Issue 4, 2022

Published on: 20 April, 2021

Page: [682 - 699] Pages: 18

DOI: 10.2174/0929867328666210420103021

Price: $65


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.

Keywords: SARS-CoV-2, COVID-19, spike protein, angiotensin-converting enzyme 2, transmembrane protease, serine 2, drug design.

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