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dc.contributor.author | Moasses Ghafary, Soroush | es_ES |
dc.contributor.author | Soriano-Teruel, Paula | es_ES |
dc.contributor.author | Lotfollahzadeh, Shima | es_ES |
dc.contributor.author | Sancho, Mónica | es_ES |
dc.contributor.author | Serrano-Candelas, Eva | es_ES |
dc.contributor.author | Karami, Fatemeh | es_ES |
dc.contributor.author | Barigye, Stephen J. | es_ES |
dc.contributor.author | Fernández-Pérez, Iván | es_ES |
dc.contributor.author | Gozalbes, Rafael | es_ES |
dc.contributor.author | Nikkhah, Maryam | es_ES |
dc.contributor.author | Orzáez, Mar | es_ES |
dc.contributor.author | Hosseinkhani, Saman | es_ES |
dc.date.accessioned | 2024-03-01T19:01:20Z | |
dc.date.available | 2024-03-01T19:01:20Z | |
dc.date.issued | 2022-01-31 | es_ES |
dc.identifier.uri | http://hdl.handle.net/10251/202882 | |
dc.description.abstract | [EN] Inflammasomes are multiprotein complexes that represent critical elements of the inflammatory response. The dysregulation of the best-characterized complex, the NLRP3 inflammasome, has been linked to the pathogenesis of diseases such as multiple sclerosis, type 2 diabetes mellitus, Alzheimer's disease, and cancer. While there exist molecular inhibitors specific for the various components of inflammasome complexes, no currently reported inhibitors specifically target NLRP3(PYD) homo-oligomerization. In the present study, we describe the identification of QM380 and QM381 as NLRP3(PYD) homo-oligomerization inhibitors after screening small molecules from the MyriaScreen library using a split-luciferase complementation assay. Our results demonstrate that these NLRP3(PYD) inhibitors interfere with ASC speck formation, inhibit pro-inflammatory cytokine IL1-beta release, and decrease pyroptotic cell death. We employed spectroscopic techniques and computational docking analyses with QM380 and QM381 and the PYD domain to confirm the experimental results and predict possible mechanisms underlying the inhibition of NLRP3(PYD) homo-interactions. | es_ES |
dc.description.sponsorship | This research was funded by EC-funded RISE (EPIC 690939), Spanish Ministry of Economy and Competitiveness, FEDER (SAF2017-84689-R), Generalitat Valenciana (PROMETEO/2019/065), research council of Tarbiat Modares University (#IG/39803). | es_ES |
dc.language | Inglés | es_ES |
dc.publisher | MDPI AG | es_ES |
dc.relation.ispartof | International Journal of Molecular Sciences | es_ES |
dc.rights | Reconocimiento (by) | es_ES |
dc.subject | Inflammasome inhibitors | es_ES |
dc.subject | NLRP3 | es_ES |
dc.subject | PYD | es_ES |
dc.subject | Screening | es_ES |
dc.subject | Split-luciferase | es_ES |
dc.subject | Pyroptosis | es_ES |
dc.title | Identification of NLRP3 PYD Homo-Oligomerization Inhibitors with Anti-Inflammatory Activity | es_ES |
dc.type | Artículo | es_ES |
dc.identifier.doi | 10.3390/ijms23031651 | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2017-84689-R/ES/DESCIFRANDO Y MODULANDO EL INTERACTOMA TRANSMEMBRANA DE LAS PROTEINAS BCL-2 COMO DIANA ANTITUMORAL/ | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/EC/H2020/690939/EU | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/GVA//PROMETEO%2F2019%2F065/ | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/TMU//IG%2F39803/ | es_ES |
dc.rights.accessRights | Abierto | es_ES |
dc.description.bibliographicCitation | Moasses Ghafary, S.; Soriano-Teruel, P.; Lotfollahzadeh, S.; Sancho, M.; Serrano-Candelas, E.; Karami, F.; Barigye, SJ.... (2022). Identification of NLRP3 PYD Homo-Oligomerization Inhibitors with Anti-Inflammatory Activity. International Journal of Molecular Sciences. 23(3):1-15. https://doi.org/10.3390/ijms23031651 | es_ES |
dc.description.accrualMethod | S | es_ES |
dc.relation.publisherversion | https://doi.org/10.3390/ijms23031651 | es_ES |
dc.description.upvformatpinicio | 1 | es_ES |
dc.description.upvformatpfin | 15 | es_ES |
dc.type.version | info:eu-repo/semantics/publishedVersion | es_ES |
dc.description.volume | 23 | es_ES |
dc.description.issue | 3 | es_ES |
dc.identifier.eissn | 1422-0067 | es_ES |
dc.identifier.pmid | 35163573 | es_ES |
dc.identifier.pmcid | PMC8835912 | es_ES |
dc.relation.pasarela | S\466230 | es_ES |
dc.contributor.funder | European Commission | es_ES |
dc.contributor.funder | Generalitat Valenciana | es_ES |
dc.contributor.funder | Tarbiat Modares University | es_ES |
dc.contributor.funder | Agencia Estatal de Investigación | es_ES |
dc.contributor.funder | European Regional Development Fund | es_ES |