1. Inhibition of ACE2-Spike Interaction by an ACE2 Binder Suppresses SARS-CoV-2 Entry.
- Author
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Shin YH, Jeong K, Lee J, Lee HJ, Yim J, Kim J, Kim S, and Park SB
- Subjects
- Animals, Antiviral Agents chemistry, COVID-19 metabolism, Chlorocebus aethiops, Drug Discovery, Humans, Protein Interaction Maps drug effects, SARS-CoV-2 physiology, Small Molecule Libraries chemistry, Small Molecule Libraries pharmacology, Vero Cells, Angiotensin-Converting Enzyme 2 metabolism, Antiviral Agents pharmacology, SARS-CoV-2 drug effects, Spike Glycoprotein, Coronavirus metabolism, Virus Internalization drug effects, COVID-19 Drug Treatment
- Abstract
The emergence of SARS-CoV-2 variants is a significant concern in developing effective therapeutics and vaccines in the middle of the ongoing COVID-19 pandemic. Here, we have identified a novel small molecule that inhibited the interactions between SARS-CoV-2 spike RBDs and ACE2 by modulating ACE2 without impairing its enzymatic activity necessary for normal physiological functions. Furthermore, the identified compounds suppressed viral infection in cultured cells by inhibiting the entry of ancestral and variant SARS-CoV-2. Our study suggests that targeting ACE2 could be a novel therapeutic strategy to inhibit SARS-CoV-2 entry into host cells and prevent the development of COVID-19., (© 2022 Wiley-VCH GmbH.)
- Published
- 2022
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