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10.1080/14756366.2018.1461856 http://scihub22266oqcxt.onion/10.1080/14756366.2018.1461856 C6009974!6009974 !29693453     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=29693453 &cmd=llinks): Failed to open stream: HTTP request failed! 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Identification of a novel small-molecule Keap1-Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy |pdf=|usr=}}{{29693453 }} gab.com Text Identification of a novel small-molecule Keap1-Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy JO: J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=29693453 #FOAvip A new Keap1-Nrf2 protein-protein interaction (PPI) inhibitor ZJ01 was identified from our compound library by fluorescence polarization assay, surface plasmon resonance, molecular docking and molecular dynamics simulation. ZJ01 could in vitro trigger Nrf2 nuclear translocation, subsequently resulting in increased mRNA levels of Nrf2 target genes HO-1 and NQO1. Meanwhile, ZJ01 suppressed LPS-induced production of ROS and the mRNA levels of pro-inflammatory cytokines TNF-?, IL-1? and IL-6 in H9c2 cardiac cells. Moreover, in an in vivo mouse model of septic cardiomyopathy induced by intraperitoneal injection of lipopolysaccharide, ZJ01 demonstrated a cytoprotective effect, upregulated Nrf2 protein nuclear accumulation, and remarkably suppressed the abovementioned cytokine levels in cardiomyocytes. The results presented herein provided a novel chemotype for the development of direct Keap1-Nrf2 PPI inhibitors and suggested that compound ZJ01 is a promising drug lead for septic cardiomyopathy treatment. ZJ01 was identified as a new Keap1-Nrf2 PPI inhibitor and drug lead for septic cardiomyopathy treatment by in vitro and in vivo experiments. Twit Text FOAVip Identification of a novel small-molecule Keap1-Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy ????J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=29693453 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=29693453 #FOAvip English Wikipedia <ref>{{Cite pmid|29693453 }}</ref> Identification of a novel small-molecule Keap1-Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy #MMPMID29693453 Jiang CS ; Zhuang CL ; Zhu K ; Zhang J ; Muehlmann LA ; Figueiró Longo JP ; Azevedo RB ; Zhang W ; Meng N ; Zhang H J Enzyme Inhib Med Chem 2018[Dec]; 33 (1 ): 833-841 PMID29693453 show ga A new Keap1-Nrf2 protein-protein interaction (PPI) inhibitor ZJ01 was identified from our compound library by fluorescence polarization assay, surface plasmon resonance, molecular docking and molecular dynamics simulation. ZJ01 could in vitro trigger Nrf2 nuclear translocation, subsequently resulting in increased mRNA levels of Nrf2 target genes HO-1 and NQO1. Meanwhile, ZJ01 suppressed LPS-induced production of ROS and the mRNA levels of pro-inflammatory cytokines TNF-?, IL-1? and IL-6 in H9c2 cardiac cells. Moreover, in an in vivo mouse model of septic cardiomyopathy induced by intraperitoneal injection of lipopolysaccharide, ZJ01 demonstrated a cytoprotective effect, upregulated Nrf2 protein nuclear accumulation, and remarkably suppressed the abovementioned cytokine levels in cardiomyocytes. The results presented herein provided a novel chemotype for the development of direct Keap1-Nrf2 PPI inhibitors and suggested that compound ZJ01 is a promising drug lead for septic cardiomyopathy treatment. ZJ01 was identified as a new Keap1-Nrf2 PPI inhibitor and drug lead for septic cardiomyopathy treatment by in vitro and in vivo experiments. |Animals [MESH] |Cardiomyopathies/chemically induced/*drug therapy/metabolism [MESH] |Cells, Cultured [MESH] |Cytokines/antagonists & inhibitors/biosynthesis [MESH] |Cytoprotection/*drug effects [MESH] |Dose-Response Relationship, Drug [MESH] |Kelch-Like ECH-Associated Protein 1/*antagonists & inhibitors/genetics/metabolism [MESH] |Lipopolysaccharides/*antagonists & inhibitors/pharmacology [MESH] |Male [MESH] |Mice [MESH] |Mice, Inbred C57BL [MESH] |Models, Molecular [MESH] |Molecular Structure [MESH] |NF-E2-Related Factor 2/*antagonists & inhibitors/genetics/metabolism [MESH] |Protein Binding/drug effects [MESH] |RNA, Messenger/antagonists & inhibitors/biosynthesis [MESH] |Rats [MESH] |Reactive Oxygen Species/antagonists & inhibitors/metabolism [MESH] |Small Molecule Libraries/chemical synthesis/chemistry/*pharmacology [MESH]Identification of a novel small-molecule Keap1-Nrf2 PPI inhibitor with(epmc).pdf DeepDyve Pubget Overpricing