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Dipeptidyl Peptidase 4 Inhibitors

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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...

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Related Experiment Video

Updated: Nov 26, 2025

Live Imaging and Quantification of Viral Infection in K18 hACE2 Transgenic Mice Using Reporter-Expressing Recombinant SARS-CoV-2

Live Imaging and Quantification of Viral Infection in K18 hACE2 Transgenic Mice Using Reporter-Expressing Recombinant SARS-CoV-2

Published on: November 5, 2021

Potential SARS-CoV-2 main protease inhibitors.

Riddhidev Banerjee¹, Lalith Perera², L M Viranga Tillekeratne¹

¹Department of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, University of Toledo, Toledo, OH 43606, USA.

Drug Discovery Today

|December 14, 2020

Summary

Researchers are actively seeking new treatments for COVID-19 by developing small-molecule inhibitors that target the SARS-CoV-2 main protease (Mpro), a crucial enzyme for viral replication.

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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

Area of Science:

Virology
Drug Discovery
Biochemistry

Background:

The COVID-19 pandemic necessitates novel therapeutic strategies against SARS-CoV-2.
Currently, no drugs specifically target SARS-CoV-2, highlighting the need for antiviral development.
The SARS-CoV-2 main protease (Mpro) is a key target for drug discovery due to its essential role in viral replication.

Purpose of the Study:

To review recent advancements in the identification of small-molecule inhibitors targeting the SARS-CoV-2 main protease (Mpro).
To explore the potential of Mpro as a therapeutic target for COVID-19 treatment.

Main Methods:

Analysis of conserved structural features of coronavirus main proteases.
Review of virtual screening and in vitro studies for Mpro inhibitor discovery.
Examination of the impact of the SARS-CoV-2 Mpro crystal structure on drug design.

Main Results:

Significant progress has been made in discovering Mpro inhibitors through various screening methods.
The conserved substrate-binding region of Mpro across different coronaviruses offers a viable target for inhibitor design.
The availability of the SARS-CoV-2 Mpro crystal structure accelerates inhibitor development.

Conclusions:

Small-molecule inhibitors targeting SARS-CoV-2 Mpro represent a promising therapeutic avenue for COVID-19.
Continued research into Mpro inhibitors is crucial for developing effective treatments against SARS-CoV-2.
The structural conservation of Mpro provides a foundation for broad-spectrum coronavirus protease inhibitor development.