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10.1089/ars.2014.6202 http://scihub22266oqcxt.onion/10.1089/ars.2014.6202 C4545375!4545375!26135714     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Antioxid+Redox+Signal 2015 ; 23 (5): 358-74 Nephropedia Template TP {{tp|p=26135714|t=2015. Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor |pdf=|usr=}}{{26135714}} gab.com Text Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor JO: Antioxid Redox Signal http://www.kidney.de/pget.php?&tw=1&pmid=26135714 #FOAvip Aims: The NADPH oxidase (NOX) family of enzymes catalyzes the formation of reactive oxygen species (ROS). NOX enzymes not only have a key role in a variety of physiological processes but also contribute to oxidative stress in certain disease states. To date, while numerous small molecule inhibitors have been reported (in particular for NOX2), none have demonstrated inhibitory activity in vivo. As such, there is a need for the identification of improved NOX inhibitors to enable further evaluation of the biological functions of NOX enzymes in vivo as well as the therapeutic potential of NOX inhibition. In this study, both the in vitro and in vivo pharmacological profiles of GSK2795039, a novel NOX2 inhibitor, were characterized in comparison with other published NOX inhibitors. Results: GSK2795039 inhibited both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. It inhibited NOX2 in an NADPH competitive manner and was selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes. Following systemic administration in mice, GSK2795039 abolished the production of ROS by activated NOX2 enzyme in a paw inflammation model. Furthermore, GSK2795039 showed activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein. Innovation and Conclusions: GSK2795039 is a novel NOX2 inhibitor that is the first small molecule to demonstrate inhibition of the NOX2 enzyme in vivo. Antioxid. Redox Signal. 23, 358?374. Twit Text FOAVip Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor ????Antioxid Redox Signal http://www.kidney.de/pget.php?&tw=1&pmid=26135714 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=26135714 #FOAvip English Wikipedia <ref>{{Cite pmid|26135714}}</ref> Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor #MMPMID26135714 Hirano K; Chen WS; Chueng AL; Dunne AA; Seredenina T; Filippova A; Ramachandran S; Bridges A; Chaudry L; Pettman G; Allan C; Duncan S; Lee KC; Lim J; Ma MT; Ong AB; Ye NY; Nasir S; Mulyanidewi S; Aw CC; Oon PP; Liao S; Li D; Johns DG; Miller ND; Davies CH; Browne ER; Matsuoka Y; Chen DW; Jaquet V; Rutter AR Antioxid Redox Signal 2015[Aug]; 23 (5): 358-74 PMID26135714show ga Aims: The NADPH oxidase (NOX) family of enzymes catalyzes the formation of reactive oxygen species (ROS). NOX enzymes not only have a key role in a variety of physiological processes but also contribute to oxidative stress in certain disease states. To date, while numerous small molecule inhibitors have been reported (in particular for NOX2), none have demonstrated inhibitory activity in vivo. As such, there is a need for the identification of improved NOX inhibitors to enable further evaluation of the biological functions of NOX enzymes in vivo as well as the therapeutic potential of NOX inhibition. In this study, both the in vitro and in vivo pharmacological profiles of GSK2795039, a novel NOX2 inhibitor, were characterized in comparison with other published NOX inhibitors. Results: GSK2795039 inhibited both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. It inhibited NOX2 in an NADPH competitive manner and was selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes. Following systemic administration in mice, GSK2795039 abolished the production of ROS by activated NOX2 enzyme in a paw inflammation model. Furthermore, GSK2795039 showed activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein. Innovation and Conclusions: GSK2795039 is a novel NOX2 inhibitor that is the first small molecule to demonstrate inhibition of the NOX2 enzyme in vivo. Antioxid. Redox Signal. 23, 358?374. äDiscovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibi(epmc).pdf DeepDyve Pubget Overpricing