• Drug-mediated intracellular donation of nitric oxide potently inhibits 5-lipoxygenase: a possible key to future antileukotriene therapy 

    Roos, Jessica; Peters, Marcus; Maucher, Isabelle V.; Kühn, Benjamin; Fettel, Jasmin; Hellmuth, Nadine; Brat, Camilla; Sommer, Benita; Urbschat, Anja; Piesche, Matthias; Vogel, Anja; Proschak, Ewgenij; Blöcher, René; Buscató, Estella; Häfner, Ann-Kathrin; Matrone, Carmela; Werz, Oliver; Heidler, Juliana; Wittig, Ilka; Angioni, Carlo; Geisslinger, Gerd; Parnham, Michael J.; Zacharowski, Kai D.; Steinhilber, Dieter; Maier, Thorsten J. (2018)
    Aims: 5-Lipoxygenase (5-LO) is the key enzyme of leukotriene (LT) biosynthesis and is critically involved in a number of inflammatory diseases such as arthritis, gout, bronchial asthma, atherosclerosis, and cancer. Because ...

  • 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 ...

  • 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. ...