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

Author:

Neukirch Konstantin12ORCID,Alsabil Khaled3,Dinh Chau-Phi3,Bilancia Rossella4,Raasch Martin5,Ville Alexia3,Cerqua Ida4,Viault Guillaume3,Bréard Dimitri3,Pace Simona2,Temml Veronika6,Brunner Elena2,Jordan Paul M.2,Marques Marta C.7,Loeser Konstantin2,Gollowitzer André12,Permann Stephan1,Gerstmeier Jana2,Lorkowski Stefan8,Stuppner Hermann9ORCID,Garscha Ulrike10,Rodrigues Tiago7,Bernardes Gonçalo J. L.711ORCID,Schuster Daniela6ORCID,Séraphin Denis3ORCID,Richomme Pascal3,Rossi Antonietta4,Mosig Alexander S.5ORCID,Roviezzo Fiorentina4,Werz Oliver2ORCID,Helesbeux Jean-Jacques3,Koeberle Andreas12ORCID

Affiliation:

1. Michael Popp Institute and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, 6020 Innsbruck, Austria

2. Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany

3. Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France

4. Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, 80131 Naples, Italy

5. Institute of Biochemistry II, Jena University Hospital, 07747 Jena, Germany

6. Department of Pharmaceutical and Medicinal Chemistry, Paracelsus Medical University Salzburg, 5020 Salzburg, Austria

7. Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, 1649-028 Lisboa, Portugal

8. Department of Nutritional Biochemistry and Physiology, Institute of Nutritional Science and Competence Cluster for Nutrition and Cardiovascular Health (nutriCARD), Halle-Jena-Leipzig, Friedrich Schiller University Jena, 07743 Jena, Germany

9. Institute of Pharmacy/Pharmacognosy and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, 6020 Innsbruck, Austria

10. Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, University of Greifswald, 17489 Greifswald, Germany

11. Department of Chemistry, University of Cambridge, CB2 1EW Cambridge, U.K.

Funder

Agence Nationale de la Recherche

Freistaat Th??ringen

Deutscher Akademischer Austauschdienst

Austrian Science Fund

Deutsche Forschungsgemeinschaft

European Social Fund

Ministero della Universit?? e della Ricerca

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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