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Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.
Terrett, Jack A; Chen, Huifen; Shore, Daniel G; Villemure, Elisia; Larouche-Gauthier, Robin; Déry, Martin; Beaumier, Francis; Constantineau-Forget, Léa; Grand-Maître, Chantal; Lépissier, Luce; Ciblat, Stéphane; Sturino, Claudio; Chen, Yong; Hu, Baihua; Lu, Aijun; Wang, Yunli; Cridland, Andrew P; Ward, Stuart I; Hackos, David H; Reese, Rebecca M; Shields, Shannon D; Chen, Jun; Balestrini, Alessia; Riol-Blanco, Lorena; Lee, Wyne P; Liu, John; Suto, Eric; Wu, Xiumin; Zhang, Juan; Ly, Justin Q; La, Hank; Johnson, Kevin; Baumgardner, Matt; Chou, Kang-Jye; Rohou, Alexis; Rougé, Lionel; Safina, Brian S; Magnuson, Steven; Volgraf, Matthew.
  • Terrett JA; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Chen H; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Shore DG; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Villemure E; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Larouche-Gauthier R; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Déry M; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Beaumier F; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Constantineau-Forget L; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Grand-Maître C; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Lépissier L; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Ciblat S; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Sturino C; Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.
  • Chen Y; Pharmaron-Beijing Co. Ltd., 6 Taihe Road, BDA, Beijing 100176, PR China.
  • Hu B; Pharmaron-Beijing Co. Ltd., 6 Taihe Road, BDA, Beijing 100176, PR China.
  • Lu A; Pharmaron-Beijing Co. Ltd., 6 Taihe Road, BDA, Beijing 100176, PR China.
  • Wang Y; Pharmaron-Beijing Co. Ltd., 6 Taihe Road, BDA, Beijing 100176, PR China.
  • Cridland AP; Charles River Laboratories, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Ward SI; Charles River Laboratories, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Hackos DH; Department of Neurosciences, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Reese RM; Department of Neurosciences, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Shields SD; Department of Neurosciences, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Chen J; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Balestrini A; Department of Discovery Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Riol-Blanco L; Department of Discovery Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Lee WP; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Liu J; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Suto E; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Wu X; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Zhang J; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Ly JQ; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • La H; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Johnson K; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Baumgardner M; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Chou KJ; Department of Small Molecule Pharmaceutical Sciences, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Rohou A; Department of Structural Biology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Rougé L; Department of Structural Biology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Safina BS; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Magnuson S; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Volgraf M; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
J Med Chem ; 64(7): 3843-3869, 2021 04 08.
Article en En | MEDLINE | ID: mdl-33749283

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Purinas / Asma / Canal Catiónico TRPA1 / Furanos Tipo de estudio: Etiology_studies Límite: Animals / Humans / Male Idioma: En Año: 2021 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Purinas / Asma / Canal Catiónico TRPA1 / Furanos Tipo de estudio: Etiology_studies Límite: Animals / Humans / Male Idioma: En Año: 2021 Tipo del documento: Article