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10.1038/s41467-016-0009-6 http://scihub22266oqcxt.onion/10.1038/s41467-016-0009-6 C5431875!5431875!28232747     free     free     free Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Nat+Commun 2017 ; 8 (ä): ä Nephropedia Template TP {{tp|p=28232747|t=2017. In situ click chemistry generation of cyclooxygenase-2 inhibitors |pdf=|usr=}}{{28232747}} gab.com Text In situ click chemistry generation of cyclooxygenase-2 inhibitors JO: Nat Commun http://www.kidney.de/pget.php?&tw=1&pmid=28232747 #FOAvip Cyclooxygenase-2 isozyme is a promising anti-inflammatory drug target, and overexpression of this enzyme is also associated with several cancers and neurodegenerative diseases. The amino-acid sequence and structural similarity between inducible cyclooxygenase-2 and housekeeping cyclooxygenase-1 isoforms present a significant challenge to design selective cyclooxygenase-2 inhibitors. Herein, we describe the use of the cyclooxygenase-2 active site as a reaction vessel for the in situ generation of its own highly specific inhibitors. Multi-component competitive-binding studies confirmed that the cyclooxygenase-2 isozyme can judiciously select most appropriate chemical building blocks from a pool of chemicals to build its own highly potent inhibitor. Herein, with the use of kinetic target-guided synthesis, also termed as in situ click chemistry, we describe the discovery of two highly potent and selective cyclooxygenase-2 isozyme inhibitors. The in vivo anti-inflammatory activity of these two novel small molecules is significantly higher than that of widely used selective cyclooxygenase-2 inhibitors. Twit Text FOAVip In situ click chemistry generation of cyclooxygenase-2 inhibitors ????Nat Commun http://www.kidney.de/pget.php?&tw=1&pmid=28232747 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=28232747 #FOAvip English Wikipedia <ref>{{Cite pmid|28232747}}</ref> In situ click chemistry generation of cyclooxygenase-2 inhibitors #MMPMID28232747 Bhardwaj A; Kaur J; Wuest M; Wuest F Nat Commun 2017[]; 8 (ä): ä PMID28232747show ga Cyclooxygenase-2 isozyme is a promising anti-inflammatory drug target, and overexpression of this enzyme is also associated with several cancers and neurodegenerative diseases. The amino-acid sequence and structural similarity between inducible cyclooxygenase-2 and housekeeping cyclooxygenase-1 isoforms present a significant challenge to design selective cyclooxygenase-2 inhibitors. Herein, we describe the use of the cyclooxygenase-2 active site as a reaction vessel for the in situ generation of its own highly specific inhibitors. Multi-component competitive-binding studies confirmed that the cyclooxygenase-2 isozyme can judiciously select most appropriate chemical building blocks from a pool of chemicals to build its own highly potent inhibitor. Herein, with the use of kinetic target-guided synthesis, also termed as in situ click chemistry, we describe the discovery of two highly potent and selective cyclooxygenase-2 isozyme inhibitors. The in vivo anti-inflammatory activity of these two novel small molecules is significantly higher than that of widely used selective cyclooxygenase-2 inhibitors. äIn situ click chemistry generation of cyclooxygenase-2 inhibitors (epmc).pdf DeepDyve Pubget Overpricing