Isabelle V Maucher, Michael Rühl, Simon B M Kretschmer, Bettina Hofmann, Benjamin Kühn, Jasmin Fettel, Anja Vogel, Karsten T Flügel, Georg Manolikakes, Nadine Hellmuth, Ann-Kathrin Häfner, Vahid Golghalyani, Ann-Katrin Ball, Matthias Piesche, Carmela Matrone, Gerd Geisslinger, Michael J Parnham, Michael Karas, Dieter Steinhilber, Jessica Roos, Thorsten J Maier
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 electrophilicity is derived from an intramolecular Michael acceptor moiety consisting of an electron-withdrawing group in close proximity to a double bond. The potential of the Michael acceptor moiety to interact with functionally relevant cysteines of proteins potentially renders them effective and sustained enzyme activity modulators...
February 1, 2017: Biochemical Pharmacology