MCC950 closes the active conformation of NLRP3 to an inactive state

NLRP3 is an innate immune sensor contributing to the development of different diseases including monogenic autoinflammatory syndromes, gout, atherosclerosis, and Alzheimer’s disease. The molecule sulfonylurea MCC950 is a NLRP3 inflammasome inhibitor with potential clinical utility. However, the mech...

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Detalles Bibliográficos
Autores principales: Tapia-Abellán, Ana, Angosto-Bazarra, Diego, Martínez-Banaclocha, Helios, de Torre-Minguela, Carlos, Cerón-Carrasco, Jose P., Pérez-Sánchez, Horacio, Arostegui, Juan I., Pelegrin, Pablo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2019
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7116292/
https://www.ncbi.nlm.nih.gov/pubmed/31086329
http://dx.doi.org/10.1038/s41589-019-0278-6
Descripción
Sumario:NLRP3 is an innate immune sensor contributing to the development of different diseases including monogenic autoinflammatory syndromes, gout, atherosclerosis, and Alzheimer’s disease. The molecule sulfonylurea MCC950 is a NLRP3 inflammasome inhibitor with potential clinical utility. However, the mechanism of action of MCC950 remains unknown. Here, we characterize the mechanism of action of MCC950 in both wild-type and autoinflammatory-related NLRP3 mutants, demonstrating that MCC950 closes the ‘open’ conformation of active NLRP3.

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