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A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation

A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation

Published on: January 9, 2019

Drug development targeting SARS-CoV-2 main protease.

¹The Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA.

Global Health & Medicine

|January 2, 2023

Summary

The SARS-CoV-2 main protease (Mpro) is crucial for viral replication and a key target for new COVID-19 therapies. This review details recent advancements in developing Mpro inhibitors to combat the ongoing pandemic.

Keywords:

COVID-19 SARS-CoV-2 drug development main protease

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Last Updated: Aug 15, 2025

A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation

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Published on: January 9, 2019

Engineering Antiviral Agents via Surface Plasmon Resonance

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Published on: November 5, 2021

Area of Science:

Virology
Drug Discovery
Medicinal Chemistry

Background:

The COVID-19 pandemic, caused by SARS-CoV-2, has resulted in millions of deaths globally.
Despite vaccines, highly contagious variants like Omicron continue to spread, necessitating further therapeutic strategies.
The SARS-CoV-2 main protease (Mpro) is essential for viral polyprotein processing, making it a prime drug target.

Purpose of the Study:

To review and summarize recent progress in the development of therapeutic drugs targeting the SARS-CoV-2 Mpro.
To highlight key findings and potential strategies for Mpro inhibitor-based COVID-19 treatments.

Main Methods:

Literature review of recent scientific publications and clinical trial data.
Analysis of studies focusing on the structure, function, and inhibition of SARS-CoV-2 Mpro.
Synthesis of information on various classes of Mpro inhibitors and their therapeutic potential.

Main Results:

Several classes of Mpro inhibitors have shown promising preclinical and clinical activity.
Drug candidates targeting Mpro have demonstrated efficacy in reducing viral load and disease severity.
Ongoing research is focused on optimizing inhibitor potency, selectivity, and pharmacokinetic properties.

Conclusions:

Therapeutic agents targeting SARS-CoV-2 Mpro represent a promising strategy to combat COVID-19.
Continued research and development are crucial for bringing effective Mpro inhibitors to the clinic.
Mpro inhibitors could play a vital role in managing current and future coronavirus outbreaks.