Inhibition of sars-cov-2 entry into host cells using small molecules

Kenana Al Adem, Aya Shanti, Cesare Stefanini, Sungmun Lee

Research output: Contribution to journalReview articlepeer-review

25 Scopus citations


Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), a virus belonging to the Coronavirus family, is now known to cause Coronavirus Disease (Covid-19) which was first recognized in December 2019. Covid-19 leads to respiratory illnesses ranging from mild infections to pneumonia and lung failure. Strikingly, within a few months of its first report, Covid-19 has spread worldwide at an exceptionally high speed and it has caused enormous human casualties. As yet, there is no specific treatment for Covid-19. Designing inhibitory drugs that can interfere with the viral entry process constitutes one of the main preventative therapies that could combat SARS-CoV-2 infection at an early stage. In this review, we provide a brief introduction of the main features of coronaviruses, discuss the entering mechanism of SARS-CoV-2 into human host cells and review small molecules that inhibit SARS-CoV-2 entry into host cells. Specifically, we focus on small molecules, identified by experimental validation and/or computational prediction, that target the SARS-CoV-2 spike protein, human angiotensin converting enzyme 2 (ACE2) receptor and the different host cell proteases that activate viral fusion. Given the persistent rise in Covid-19 cases to date, efforts should be directed towards validating the therapeutic effectiveness of these identified small molecule inhibitors.

Original languageBritish English
Article number447
Pages (from-to)1-34
Number of pages34
Issue number12
StatePublished - Dec 2020


  • Angiotensin converting enzyme 2
  • Covid-19
  • Inhibitors
  • SARS-CoV-2
  • Small molecule
  • Spike protein


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