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Related Experiment Video

Updated: Jul 27, 2025

Author Spotlight: Developing Tools to Tune the Activity of Tyrosine Phosphatases

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TMPRSS2 Inhibitor Discovery Facilitated through an In Silico and Biochemical Screening Platform.

Amanda L Peiffer^1,2, Julie M Garlick^1,3, Yujin Wu³

¹Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48019, United States.

ACS Medicinal Chemistry Letters

|June 7, 2023

Summary

New antiviral strategies are needed for COVID-19. Researchers identified debrisoquine as a promising noncovalent inhibitor of transmembrane serine protease 2 (TMPRSS2), blocking SARS-CoV-2 entry and infectivity.

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Area of Science:

Biochemistry
Virology
Drug Discovery

Background:

The COVID-19 pandemic necessitates novel antiviral therapies due to the ineffectiveness of current drugs against SARS-CoV-2.
The host transmembrane serine protease, TMPRSS2, is a key target for antiviral development as it facilitates viral entry by priming the spike protein.

Purpose of the Study:

To identify novel noncovalent inhibitors of TMPRSS2 using virtual screening and biochemical assays.
To evaluate the efficacy of identified inhibitors in blocking SARS-CoV-2 infectivity in a cellular model.

Main Methods:

Virtual screening of compound libraries to identify potential TMPRSS2 inhibitors.
Optimization of recombinant TMPRSS2 peptidase domain expression and purification.
Biochemical kinetic assays for inhibitor characterization.
Cellular assays to assess SARS-CoV-2 infectivity inhibition.

Main Results:

Identification of a focused collection of potential TMPRSS2 inhibitors.
Discovery of new noncovalent TMPRSS2 inhibitors demonstrating efficacy in blocking SARS-CoV-2 infectivity.
Debrisoquine identified as a potent inhibitor with high ligand efficiency and tractability for further development.

Conclusions:

Noncovalent TMPRSS2 inhibitors represent a viable therapeutic strategy against SARS-CoV-2.
Debrisoquine is a promising hit compound for developing new antiviral agents targeting TMPRSS2.