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Peroxide derivatives as SARS-CoV-2 entry inhibitors
Ding-Qi Zhang1, Qin-Hai Ma2, Meng-Chu Yang1
1Dr. Neher's Biophysics Laboratory for Innovative Drug Discovery, State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Macau, China.
Virus Research
|December 11, 2023
Summary
Researchers identified two peroxide compounds that inhibit the interaction between the SARS-CoV-2 spike protein and ACE2, blocking viral entry and showing potential as COVID-19 therapeutics.
Area of Science:
- Biochemistry
- Virology
- Medicinal Chemistry
Background:
- Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes the COVID-19 pandemic.
- Viral entry into host cells involves the spike protein (S) binding to human angiotensin-converting enzyme 2 (ACE2) via its receptor-binding domain (RBD).
Purpose of the Study:
- To screen small molecules for their ability to inhibit the RBD-ACE2 interaction.
- To identify potential therapeutic agents against SARS-CoV-2.
Main Methods:
- Bio-layer interferometry (BLI) was employed to screen 52 peroxides.
- Inhibition of SARS-CoV-2 cell entry was assessed using pseudovirus and authentic SARS-CoV-2 assays.
- In silico analysis evaluated physicochemical and pharmacokinetic properties.
Main Results:
- Two compounds, designated 21 and 29, effectively inhibited the RBD-ACE2 interaction.
- Compounds 21 and 29 demonstrated inhibition of SARS-CoV-2 cell entry.
- In silico analysis indicated favorable physicochemical and pharmacokinetic profiles for both compounds.
Conclusions:
- Small molecules targeting the RBD-ACE2 interaction show promise as COVID-19 therapeutics.
- Compounds 21 and 29 represent potential drug candidates for treating COVID-19.
