Browsing by Subject "Mechanism of action"
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- PublicationOpen AccessMCC950 closes the active conformation of NLRP3 to an inactive state(Nature Research, 2019-06) Angosto-Bazarra, Diego; Martínez-Banaclocha, Helios; Torre-Minguela, Carlos de; Cerón-Carrasco, Jose P; Pérez-Sánchez, Horacio; Arostegui, Juan I; Pelegrín Vivancos, Pablo; Tapia Abellán, Ana; Bioquímica y Biología Molecular B e InmunologíaNLRP3 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.