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Inhibitors of SARS-CoV-2 Entry: Current and Future Opportunities

  • Xiu, Siyu1
  • Dick, Alexej2
  • Ju, Han1
  • Mirzaie, Sako3
  • Abdi, Fatemeh3
  • Cocklin, Simon2
  • Zhan, Peng1
  • Liu, Xinyong1
  • 1 Shandong University, China , (China)
  • 2 Drexel University College of Medicine, United States , (United States)
  • 3 Islamic Azad University, Iran
Published Article
Journal of Medicinal Chemistry
American Chemical Society
Publication Date
Jun 15, 2020
DOI: 10.1021/acs.jmedchem.0c00502
PMID: 32539378
PMCID: PMC7315836
PubMed Central


Recently, a novel coronavirus initially designated 2019-nCoV but now termed SARS-CoV-2 has emerged and raised global concerns due to its virulence. SARS-CoV-2 is the etiological agent of “coronavirus disease 2019”, abbreviated to COVID-19, which despite only being identified at the very end of 2019, has now been classified as a pandemic by the World Health Organization (WHO). At this time, no specific prophylactic or postexposure therapy for COVID-19 are currently available. Viral entry is the first step in the SARS-CoV-2 lifecycle and is mediated by the trimeric spike protein. Being the first stage in infection, entry of SARS-CoV-2 into host cells is an extremely attractive therapeutic intervention point. Within this review, we highlight therapeutic intervention strategies for anti-SARS-CoV, MERS-CoV, and other coronaviruses and speculate upon future directions for SARS-CoV-2 entry inhibitor designs.

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