Action of Dipeptidyl Peptidase-4 Inhibitors on SARS-CoV-2 Main Protease.
ChemMedChem
; 16(9): 1425-1426, 2021 05 06.
Article
in English
| MEDLINE | ID: covidwho-985986
ABSTRACT
In a recent publication, Eleftheriou etâ
al. proposed that inhibitors of dipeptidyl peptidase-4 (DPP-4) are functional inhibitors of the main protease (Mpro ) of SARS-CoV-2. Their predictions prompted the authors to suggest linagliptin, a DPP-4 inhibitor and approved anti-diabetes drug, as a repurposed drug candidate against the ongoing COVID-19 pandemic. We used an enzymatic assay measuring the inhibition of Mpro catalytic activity in the presence of four different commercially available gliptins (linagliptin, sitagliptin, alogliptin and saxagliptin) and several structural analogues of linagliptin to study the binding of DPP-4 inhibitors to Mpro and their functional activity. We show here that DPP-4 inhibitors like linagliptin, other gliptins and structural analogues are inactive against Mpro .
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Dipeptidyl-Peptidase IV Inhibitors
/
Drug Repositioning
/
Coronavirus 3C Proteases
/
SARS-CoV-2
/
Heterocyclic Compounds
Type of study:
Prognostic study
Language:
English
Journal:
ChemMedChem
Journal subject:
Pharmacology
/
Chemistry
Year:
2021
Document Type:
Article
Affiliation country:
Cmdc.202000921
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