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Page 1
Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation.
Neukirch K, Alsabil K, Dinh CP, Bilancia R, Raasch M, Ville A, Cerqua I, Viault G, Bréard D, Pace S, Temml V, Brunner E, Jordan PM, Marques MC, Loeser K, Gollowitzer A, Permann S, Gerstmeier J, Lorkowski S, Stuppner H, Garscha U, Rodrigues T, Bernardes GJL, Schuster D, Séraphin D, Richomme P, Rossi A, Mosig AS, Roviezzo F, Werz O, Helesbeux JJ, Koeberle A. Neukirch K, et al. J Med Chem. 2021 Aug 12;64(15):11496-11526. doi: 10.1021/acs.jmedchem.1c00806. Epub 2021 Jul 19. J Med Chem. 2021. PMID: 34279935 Free PMC article.
Endogenous metabolites of vitamin E limit inflammation by targeting 5-lipoxygenase.
Pein H, Ville A, Pace S, Temml V, Garscha U, Raasch M, Alsabil K, Viault G, Dinh CP, Guilet D, Troisi F, Neukirch K, König S, Bilancia R, Waltenberger B, Stuppner H, Wallert M, Lorkowski S, Weinigel C, Rummler S, Birringer M, Roviezzo F, Sautebin L, Helesbeux JJ, Séraphin D, Mosig AS, Schuster D, Rossi A, Richomme P, Werz O, Koeberle A. Pein H, et al. Among authors: neukirch k. Nat Commun. 2018 Sep 20;9(1):3834. doi: 10.1038/s41467-018-06158-5. Nat Commun. 2018. PMID: 30237488 Free PMC article.
A vitamin E long-chain metabolite and the inspired drug candidate α-amplexichromanol relieve asthma features in an experimental model of allergen sensitization.
Cerqua I, Neukirch K, Terlizzi M, Granato E, Caiazzo E, Cicala C, Ialenti A, Capasso R, Werz O, Sorrentino R, Seraphin D, Helesbeux JJ, Cirino G, Koeberle A, Roviezzo F, Rossi A. Cerqua I, et al. Among authors: neukirch k. Pharmacol Res. 2022 Jul;181:106250. doi: 10.1016/j.phrs.2022.106250. Epub 2022 May 10. Pharmacol Res. 2022. PMID: 35562015
Learning from Nature: From a Marine Natural Product to Synthetic Cyclooxygenase-1 Inhibitors by Automated De Novo Design.
Friedrich L, Cingolani G, Ko YH, Iaselli M, Miciaccia M, Perrone MG, Neukirch K, Bobinger V, Merk D, Hofstetter RK, Werz O, Koeberle A, Scilimati A, Schneider G. Friedrich L, et al. Among authors: neukirch k. Adv Sci (Weinh). 2021 Aug;8(16):e2100832. doi: 10.1002/advs.202100832. Epub 2021 Jun 27. Adv Sci (Weinh). 2021. PMID: 34176236 Free PMC article.
PI(18:1/18:1) is a SCD1-derived lipokine that limits stress signaling.
Thürmer M, Gollowitzer A, Pein H, Neukirch K, Gelmez E, Waltl L, Wielsch N, Winkler R, Löser K, Grander J, Hotze M, Harder S, Döding A, Meßner M, Troisi F, Ardelt M, Schlüter H, Pachmayr J, Gutiérrez-Gutiérrez Ó, Rudolph KL, Thedieck K, Schulze-Späte U, González-Estévez C, Kosan C, Svatoš A, Kwiatkowski M, Koeberle A. Thürmer M, et al. Among authors: neukirch k. Nat Commun. 2022 May 27;13(1):2982. doi: 10.1038/s41467-022-30374-9. Nat Commun. 2022. PMID: 35624087 Free PMC article.