Discovery of benzo[cd]indol-2-one and benzylidene-thiazolidine-2,4-dione as new classes of NLRP3 inflammasome inhibitors via ER-β structure based virtual screening.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103500
Abstract: The structure-guided virtual screening (VS) has proved to be successful strategy in identification of new scaffolds for biological targets. The overactivity of NLRP3 inflammasome has been implicated in variety of inflammatory diseases including Alzheimer's disease.… read more here.
Keywords: virtual screening; inflammasome inhibitors; inhibitors via; structure ... See more keywords
Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113417
Abstract: NLRP3 inflammasome activation plays a critical role in inflammation and its related disorders. Herein we report a hit-to-lead effort resulting in the discovery of a novel and potent class of NLRP3 inflammasome inhibitors. Among these,… read more here.
Keywords: inflammasome inhibitors; analogues novel; inflammation; discovery chalcone ... See more keywords
Novel Aryl Sulfonamide Derivatives as NLRP3 Inflammasome Inhibitors for the Potential Treatment of Cancer.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00175
Abstract: The NLRP3 inflammasome is a critical component of innate immunity that senses diverse pathogen- and host-derived molecules. However, its aberrant activation has been associated with the pathogenesis of multiple diseases, including cancer. In this study,… read more here.
Keywords: aryl sulfonamide; sulfonamide derivatives; chemistry; inflammasome inhibitors ... See more keywords
Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00242
Abstract: The NLRP3 inflammasome is a multiprotein complex that facilitates activation and release of the proinflammatory cytokines interleukin-1β (IL-1β) and IL-18 in response to infection or endogenous stimuli. It can be inappropriately activated by a range… read more here.
Keywords: triazolopyrimidinone derivatives; derivatives selective; optimization triazolopyrimidinone; discovery optimization ... See more keywords
Putative Therapeutic Impact of Inflammasome Inhibitors against COVID-19-Induced ARDS.
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DOI: 10.2174/0929867329666220906111550
Abstract: Given the importance of COVID-19-induced ARDS, recently, researchers have strived to determine underlying mechanisms involved in the inflammatory responses. In this regard, inflammasomes possess a distinct priority for cytokine storm occurrence and subsequently ARDS progression… read more here.
Keywords: therapeutic impact; inflammasome inhibitors; putative therapeutic; covid induced ... See more keywords
Promise of the NLRP3 Inflammasome Inhibitors in In Vivo Disease Models
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DOI: 10.3390/molecules26164996
Abstract: Nucleotide-binding oligomerization domain NOD-like receptors (NLRs) are conserved cytosolic pattern recognition receptors (PRRs) that track the intracellular milieu for the existence of infection, disease-causing microbes, as well as metabolic distresses. The NLRP3 inflammasome agglomerates are… read more here.
Keywords: inflammasome inhibitors; inhibitors vivo; vivo disease; nlrp3 inflammasome ... See more keywords