Action of dipeptidyl peptidase-4 inhibitors on SARS-CoV-2 main protease.

Action of dipeptidyl peptidase-4 inhibitors on SARS-CoV-2 main protease.
ChemMedChem. 2020 Dec 21;:
Authors: Klein T, Nar H, Schnapp G, Hucke O, Hardman TC
Abstract
In a recent publication in this journal Eleftheriou et al. proposed inhibitors of dipeptidyl peptidase-4 (DPP-4) to be 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 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 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 .
PMID: 33348462 [PubMed - as supplied by publisher]

Source: ChemMedChem - December 21, 2020 Category: Chemistry Authors: Klein T, Nar H, Schnapp G, Hucke O, Hardman TC Tags: ChemMedChem Source Type: research