Crystal Structure of NLRP3 NACHT Domain With an Inhibitor Defines Mechanism of Inflammasome Inhibition

[Display omitted] •Molecular details of NLRP3 inflammasome activation/inhibition are not well understood.•The crystal structure of the NACHT domain reveals the auto-inhibited state of NLRP3.•An MCC950-like NLRP3 inhibitor locks the NACHT domain in an inactive conformation.•The work provides structur...

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Veröffentlicht in:	Journal of molecular biology 2021-12, Vol.433 (24), p.167309-167309, Article 167309
Hauptverfasser:	Dekker, Carien, Mattes, Henri, Wright, Michael, Boettcher, Andreas, Hinniger, Alexandra, Hughes, Nicola, Kapps-Fouthier, Sandra, Eder, Jörg, Erbel, Paulus, Stiefl, Nikolaus, Mackay, Angela, Farady, Christopher J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Catalytic Domain crystal structure Crystallography, X-Ray Furans - chemistry Furans - pharmacology gain-of-function Humans Indenes - chemistry Indenes - pharmacology Inflammasomes - antagonists & inhibitors Inflammasomes - metabolism inhibition MCC950 NLR Family, Pyrin Domain-Containing 3 Protein - antagonists & inhibitors NLR Family, Pyrin Domain-Containing 3 Protein - chemistry NLRP3 Inflammasome Protein Domains Sulfonamides - chemistry Sulfonamides - pharmacology
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