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Michael acceptor containing drugs are a novel class of 5-lipoxygenase inhibitor targeting the surface cysteines C416 and C418
Piesche, Matthias; Maucher, Isabelle V.; Rühl, Michael; Kretschmer, Simon B.M.; Hofmann, Bettina; Kühn, Benjamin; Fettel, Jasmin; Vogel, Anja; Flügel, Karsten T.; Manolikakes, Georg; Hellmuth, Nadine; Häfner, Ann-Kathrin; Golghalyani, Vahid; Ball, Ann-Katrin; Matrone, Carmela; Geisslinger, Gerd; Parnham, Michael J.; Karas, Michael; Steinhilber, Dieter; Roos, Jessica; Maier, Thorsten J. (2017)Recently, we published that nitro-fatty acids (NFA) are potent electrophilic molecules which inhibit 5-lipoxygenase (5-LO) by interacting catalytically with cysteine residues next to a substrate entry channel. The ...
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The emerging therapeutic potential of nitro fatty acids and other michael acceptor-containing drugs for the treatment of inflammation and cancer
Piesche, Matthias; Roos, Jessica; Kühn, Benjamin; Fettel, Jasmin; Hellmuth, Nadine; Brat, Camilla; Maucher, Isabelle V.; Awad, Omar; Matrone, Carmela; Comerma-Steffensen, Simon G.; Manolikakes, Georg; Heinicke, Ulrike; Zacharowski, Kai D.; Steinhilber, Dieter; Maier, Thorsten J. (2020)Nitro fatty acids (NFAs) are endogenously generated lipid mediators deriving from reactions of unsaturated electrophilic fatty acids with reactive nitrogen species. Furthermore, Mediterranean diets can be a source of NFA. ...