Aromatic sulphonamides of aziridine-2-carboxylic acid derivatives as novel PDIA1 and PDIA3 inhibitors.
Disulphide
PDI
aziridine
inhibitor
isomerase
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2023
Dec 2023
Historique:
medline:
19
4
2023
entrez:
18
4
2023
pubmed:
19
4
2023
Statut:
ppublish
Résumé
In this study, we report a series of newly synthesised sulphonamides of aziridine-2-carboxylic acid (Az-COOH) ester and amide analogues as potent protein disulphide isomerase (PDI, EC 5.3.4.1) inhibitors. The inhibitory activity on PDI was determined against recombinant human PDIA1 and PDIA3 proteins using an insulin reduction assay. These compounds in low micromolar to low nanomolar concentrations showed the effective
Identifiants
pubmed: 37070480
doi: 10.1080/14756366.2022.2158187
pmc: PMC10120451
doi:
Substances chimiques
aziridine-2-carboxylic acid
54080-06-7
Aziridines
0
PDIA3 protein, human
EC 5.3.4.1.
Protein Disulfide-Isomerases
EC 5.3.4.1
Sulfonamides
0
P4HB protein, human
EC 5.3.4.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2158187Références
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