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Action of Dipeptidyl Peptidase‐4 Inhibitors on SARS‐CoV‐2 Main Protease
Author(s) -
Nar Herbert,
Schnapp Gisela,
Hucke Oliver,
Hardman Timothy C.,
Klein Thomas
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202000921
Subject(s) - linagliptin , saxagliptin , alogliptin , sitagliptin , dipeptidyl peptidase 4 , dipeptidyl peptidase , pharmacology , chemistry , protease , drug repositioning , drug , enzyme , diabetes mellitus , biochemistry , medicine , metformin , type 2 diabetes , endocrinology
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 .