Action of Dipeptidyl Peptidase-4 Inhibitors on SARS-CoV-2 Main Protease.

Autor: Nar H; Boehringer-Ingelheim Pharma, GmbH & Co. KG, Birkendorferstr. 65, 88397 Biberach, Germany., Schnapp G; Boehringer-Ingelheim Pharma, GmbH & Co. KG, Birkendorferstr. 65, 88397 Biberach, Germany., Hucke O; Boehringer-Ingelheim Pharma, GmbH & Co. KG, Birkendorferstr. 65, 88397 Biberach, Germany., Hardman TC; Niche Science & Technology Ltd., 26 Bardolph Road, Richmond, Surrey, UK., Klein T; Boehringer-Ingelheim Pharma, GmbH & Co. KG, Birkendorferstr. 65, 88397 Biberach, Germany.
Jazyk: angličtina
Zdroj: ChemMedChem [ChemMedChem] 2021 May 06; Vol. 16 (9), pp. 1425-1426. Date of Electronic Publication: 2021 Feb 17.
DOI: 10.1002/cmdc.202000921
Abstrakt: In a recent publication, Eleftheriou et al. proposed that inhibitors of dipeptidyl peptidase-4 (DPP-4) are functional inhibitors of the main protease (M pro ) 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 M pro 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 M pro and their functional activity. We show here that DPP-4 inhibitors like linagliptin, other gliptins and structural analogues are inactive against M pro .
(© 2020 The Authors. Published by Wiley-VCH GmbH.)
Databáze: MEDLINE
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