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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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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:
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
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author 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
author_facet 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
author_sort Tapia-Abellán, Ana
collection PubMed
description 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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spelling pubmed-71162922020-11-03 MCC950 closes the active conformation of NLRP3 to an inactive state 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 Nat Chem Biol Article 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. 2019-06-01 2019-05-13 /pmc/articles/PMC7116292/ /pubmed/31086329 http://dx.doi.org/10.1038/s41589-019-0278-6 Text en Users may view, print, copy, and download text and data-mine the content in such documents, for the purposes of academic research, subject always to the full Conditions of use:http://www.nature.com/authors/editorial_policies/license.html#terms
spellingShingle Article
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
MCC950 closes the active conformation of NLRP3 to an inactive state
title MCC950 closes the active conformation of NLRP3 to an inactive state
title_full MCC950 closes the active conformation of NLRP3 to an inactive state
title_fullStr MCC950 closes the active conformation of NLRP3 to an inactive state
title_full_unstemmed MCC950 closes the active conformation of NLRP3 to an inactive state
title_short MCC950 closes the active conformation of NLRP3 to an inactive state
title_sort mcc950 closes the active conformation of nlrp3 to an inactive state
topic Article
url 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
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