Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Simon B.M. Kretschmer"'
Autor:
Bettina Hofmann, Kerstin Hiesinger, Steffen Brunst, Timon Eckes, Carlo Angioni, Ewgenij Proschak, Dieter Steinhilber, Jan S. Kramer, Manfred Schubert-Zsilavecz, Gerd Geisslinger, Achim Schmidtko, Josef Pfeilschifter, Simon B.M. Kretschmer, Lilia Weizel, Sandra K. Wittmann, Sven George, Stephanie Schwalm, Sandra Beyer, Jan Heering, Cathrin Flauaus, Astrid Kaiser, Denys Pogoryelov
Publikováno v:
Journal of medicinal chemistry. 63(20)
Inhibition of multiple enzymes of the arachidonic acid cascade leads to synergistic anti-inflammatory effects. Merging of 5-lipoxygenase (5-LOX) and soluble epoxide hydrolase (sEH) pharmacophores led to the discovery of a dual 5-LOX/sEH inhibitor, wh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26385089e4d61a587bead1300d2e0028
https://pubmed.ncbi.nlm.nih.gov/33044073
https://pubmed.ncbi.nlm.nih.gov/33044073
Autor:
Carlo Angioni, Bettina Hofmann, Felix F Lillich, Manfred Schubert-Zsilavecz, Jessica Roos, Stefano Woltersdorf, Holger Stark, Michael Rühl, Mario Wurglics, Ann-Kathrin Häfner, Dieter Steinhilber, Simon B.M. Kretschmer, Dominik Vogt, Michael Karas, Astrid Kaiser, Gerd Geisslinger, Isabelle V. Maucher
Publikováno v:
Biochemical Pharmacology. 123:52-62
5-Lipoxygenase (5-LO, EC1.13.11.34) has been implicated in the pathogenesis of inflammatory and immune diseases. Recently, aminothiazole comprising inhibitors have been discovered for this valuable target. Yet, the molecular mode of action of this cl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3e0eced889b420814620a56997b5620
https://doi.org/10.1016/j.bcp.2016.09.021
https://doi.org/10.1016/j.bcp.2016.09.021
Autor:
Stefano Woltersdorf, Dominik Vogt, Holger Stark, Simon B.M. Kretschmer, Ann-Kathrin Häfner, Bettina Hofmann, Dieter Steinhilber, Carmen B. Rödl
Publikováno v:
Future Medicinal Chemistry. 8:149-164
Background: Leukotrienes are pivotal lipid mediators in various immune and inflammatory reactions. Herein, 5-LO is a validated target. 2-Aminothiazoles, as a privileged structure, implicate known 5-LO inhibitors like ST-1083 (IC50 [polymorphonuclear
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bebf95f0118207cbb0a999890613f4e2
https://doi.org/10.4155/fmc.15.174
https://doi.org/10.4155/fmc.15.174
Autor:
Carmela Matrone, Vahid Golghalyani, Isabelle V. Maucher, Michael Rühl, Nadine Hellmuth, Jessica Roos, Matthias Piesche, Ann-Katrin Ball, Michael Karas, Simon B.M. Kretschmer, Ann-Kathrin Häfner, Bettina Hofmann, Georg Manolikakes, Anja Vogel, Benjamin Kühn, Gerd Geisslinger, Thorsten J. Maier, Dieter Steinhilber, Karsten T. Flügel, Jasmin Fettel, Michael J. Parnham
Publikováno v:
Maucher, I V, Rühl, M, Bm Kretschmer, S, Hofmann, B, Kühn, B, Fettel, J, Vogel, A, Flügel, K T, Manolikakes, G, Hellmuth, N, Häfner, A-K, Golghalyani, V, Ball, A-K, Piesche, M, Matrone, C, Geisslinger, G, Parnham, M J, Karas, M, Steinhilber, D, Roos, J & Maier, T J 2017, ' Michael acceptor containing drugs are a novel class of 5-lipoxygenase inhibitor targeting the surface cysteines C416 and C418 ', Biochemical Pharmacology, vol. 125, no. 1, pp. 55–74 . https://doi.org/10.1016/j.bcp.2016.11.004
Recently, we published that nitro-fatty acids (NFA) are potent electrophilic molecules which inhibit 5-lipoxygenase (5-LO) by interacting with catalytically cysteine residues next to a substrate entry channel. The electrophilicity is derived from an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a4ad1c8a0f902beeef1909da6d7f352
https://publica.fraunhofer.de/handle/publica/252024
https://publica.fraunhofer.de/handle/publica/252024
Autor:
Ewgenij Proschak, Bettina Hofmann, Sebastian Barzen, Simon B.M. Kretschmer, Astrid Brüggerhoff, Janosch Achenbach, Dieter Steinhilber, Holger Stark, Dominik Vogt, Carmen B. Rödl, Katja Ihlefeld
Publikováno v:
European Journal of Medicinal Chemistry. 84:302-311
Eicosanoids like leukotrienes and prostaglandins play a considerable role in inflammation. Produced within the arachidonic acid (AA) cascade, these lipid mediators are involved in the pathogenesis of pain as well as acute and chronic inflammatory dis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c055d16a024bee48ba1412b3ac0fe79
https://doi.org/10.1016/j.ejmech.2014.07.025
https://doi.org/10.1016/j.ejmech.2014.07.025
Autor:
Ewgenij Proschak, Daniel K. Glatzel, Karin Meirer, Bettina Hofmann, Sandra K. Wittmann, René Blöcher, Robert Fürst, Gerd Geisslinger, Markus Hartmann, Dieter Steinhilber, Simon B.M. Kretschmer, Carlo Angioni
Publikováno v:
Molecules, Vol 22, Iss 1, p 45 (2016)
Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
The arachidonic acid cascade is a key player in inflammation, and numerous well-established drugs interfere with this pathway. Previous studies have suggested that simultaneous inhibition of 5-lipoxygenase (5-LO) and soluble epoxide hydrolase (sEH) r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b0d3f9e35d4b002baee3bc0d5ed2c12
https://doi.org/10.3390/molecules22010045
https://doi.org/10.3390/molecules22010045
Autor:
Ewgenij Proschak, René Blöcher, Bettina Hofmann, Daniel Moser, Björn Krüger, Frank Löhr, Janosch Achenbach, Franca-Maria Klingler, Ann-Kathrin Häfner, Holger Stark, Dieter Steinhilber, Carmen B. Rödl, Simon B.M. Kretschmer
Design of multitarget drugs and polypharmacological compounds has become popular during the past decade. However, the main approach to design such compounds is to link two selective ligands via a flexible linker. Although such chimeric ligands often
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f2287dcddb1b53da8fdac2a2a2762d2
https://europepmc.org/articles/PMC4027374/
https://europepmc.org/articles/PMC4027374/