Identification of NLRP3^PYD Homo-Oligomerization Inhibitors with Anti-Inflammatory Activity.

ABSTRACT: 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

SUBMITTER: Moasses Ghafary S 

PROVIDER: S-EPMC8835912 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature