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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, Konstantin; Alsabil, Khaled; Dinh, Chau-Phi; Bilancia, Rossella; Raasch, Martin; Ville, Alexia; Cerqua, Ida; Viault, Guillaume; Bréard, Dimitri; Pace, Simona; Temml, Veronika; Brunner, Elena; Jordan, Paul M; Marques, Marta C; Loeser, Konstantin; Gollowitzer, André; Permann, Stephan; Gerstmeier, Jana; Lorkowski, Stefan; Stuppner, Hermann; Garscha, Ulrike; Rodrigues, Tiago; Bernardes, Gonçalo J L; Schuster, Daniela; Séraphin, Denis; Richomme, Pascal; Rossi, Antonietta; Mosig, Alexander S; Roviezzo, Fiorentina; Werz, Oliver; Helesbeux, Jean-Jacques; Koeberle, Andreas.
Affiliation
  • Neukirch K; Michael Popp Institute and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, 6020 Innsbruck, Austria.
  • Alsabil K; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany.
  • Dinh CP; Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
  • Bilancia R; Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
  • Raasch M; Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, 80131 Naples, Italy.
  • Ville A; Institute of Biochemistry II, Jena University Hospital, 07747 Jena, Germany.
  • Cerqua I; Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
  • Viault G; Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, 80131 Naples, Italy.
  • Bréard D; Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
  • Pace S; Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
  • Temml V; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany.
  • Brunner E; Department of Pharmaceutical and Medicinal Chemistry, Paracelsus Medical University Salzburg, 5020 Salzburg, Austria.
  • Jordan PM; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany.
  • Marques MC; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany.
  • Loeser K; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, 1649-028 Lisboa, Portugal.
  • Gollowitzer A; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany.
  • Permann S; Michael Popp Institute and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, 6020 Innsbruck, Austria.
  • Gerstmeier J; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany.
  • Lorkowski S; Michael Popp Institute and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, 6020 Innsbruck, Austria.
  • Stuppner H; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany.
  • Garscha U; 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.
  • Rodrigues T; Institute of Pharmacy/Pharmacognosy and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, 6020 Innsbruck, Austria.
  • Bernardes GJL; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, University of Greifswald, 17489 Greifswald, Germany.
  • Schuster D; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, 1649-028 Lisboa, Portugal.
  • Séraphin D; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, 1649-028 Lisboa, Portugal.
  • Richomme P; Department of Chemistry, University of Cambridge, CB2 1EW Cambridge, U.K.
  • Rossi A; Department of Pharmaceutical and Medicinal Chemistry, Paracelsus Medical University Salzburg, 5020 Salzburg, Austria.
  • Mosig AS; Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
  • Roviezzo F; Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
  • Werz O; Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, 80131 Naples, Italy.
  • Helesbeux JJ; Institute of Biochemistry II, Jena University Hospital, 07747 Jena, Germany.
  • Koeberle A; Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, 80131 Naples, Italy.
J Med Chem ; 64(15): 11496-11526, 2021 08 12.
Article in En | MEDLINE | ID: mdl-34279935
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Vitamin E / Arachidonate 5-Lipoxygenase / Lipoxygenase Inhibitors / Drug Discovery / Inflammation Limits: Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Document type: Article Affiliation country: Country of publication:
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Vitamin E / Arachidonate 5-Lipoxygenase / Lipoxygenase Inhibitors / Drug Discovery / Inflammation Limits: Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Document type: Article Affiliation country: Country of publication: