MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition.

Détails

ID Serval
serval:BIB_DDFDF18FD7ED
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Titre
MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition.
Périodique
Nature chemical biology
Auteur(s)
Coll R.C., Hill J.R., Day C.J., Zamoshnikova A., Boucher D., Massey N.L., Chitty J.L., Fraser J.A., Jennings M.P., Robertson AAB, Schroder K.
ISSN
1552-4469 (Electronic)
ISSN-L
1552-4450
Statut éditorial
Publié
Date de publication
06/2019
Peer-reviewed
Oui
Volume
15
Numéro
6
Pages
556-559
Langue
anglais
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't
Publication Status: ppublish
Résumé
Inhibition of the NLRP3 inflammasome is a promising strategy for the development of new treatments for inflammatory diseases. MCC950 is a potent and specific small-molecule inhibitor of the NLRP3 pathway, but its molecular target is not defined. Here, we show that MCC950 directly interacts with the Walker B motif within the NLRP3 NACHT domain, thereby blocking ATP hydrolysis and inhibiting NLRP3 activation and inflammasome formation.
Mots-clé
Adenosine Triphosphate/antagonists & inhibitors, Adenosine Triphosphate/metabolism, Binding Sites/drug effects, Heterocyclic Compounds, 4 or More Rings/chemistry, Heterocyclic Compounds, 4 or More Rings/pharmacology, Humans, Hydrolysis/drug effects, Inflammasomes/antagonists & inhibitors, Inflammasomes/biosynthesis, NLR Family, Pyrin Domain-Containing 3 Protein/antagonists & inhibitors, NLR Family, Pyrin Domain-Containing 3 Protein/metabolism, Sulfones/chemistry, Sulfones/pharmacology
Pubmed
Web of science
Création de la notice
03/06/2019 7:19
Dernière modification de la notice
20/08/2019 16:02
Données d'usage