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Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
Halkina, Tamara; Henderson, Jaclyn L; Lin, Edward Y; Himmelbauer, Martin K; Jones, J Howard; Nevalainen, Marta; Feng, Jun; King, Kristopher; Rooney, Michael; Johnson, Joshua L; Marcotte, Douglas J; Chodaparambil, Jayanth V; Kumar, P Rajesh; Patterson, Thomas A; Murugan, Paramasivam; Schuman, Eli; Wong, LaiYee; Hesson, Thomas; Lamore, Sarah; Bao, Channa; Calhoun, Michael; Certo, Hannah; Amaral, Brenda; Dillon, Gregory M; Gilfillan, Rab; de Turiso, Felix Gonzalez-Lopez.
Afiliação
  • Halkina T; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Henderson JL; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Lin EY; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Himmelbauer MK; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Jones JH; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Nevalainen M; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Feng J; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • King K; Department of Drug Metabolism and Pharmacokinetics, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Rooney M; Department of Drug Metabolism and Pharmacokinetics, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Johnson JL; Department of Drug Metabolism and Pharmacokinetics, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Marcotte DJ; Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Chodaparambil JV; Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Kumar PR; Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Patterson TA; Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Murugan P; Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Schuman E; Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Wong L; Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Hesson T; Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Lamore S; Department of Preclinical Safety, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Bao C; Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Calhoun M; Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Certo H; Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Amaral B; Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Dillon GM; Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • Gilfillan R; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
  • de Turiso FG; Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
J Med Chem ; 64(9): 6358-6380, 2021 05 13.
Article em En | MEDLINE | ID: mdl-33944571

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Encéfalo / Desenho de Fármacos / Proteínas tau / Proteínas Serina-Treonina Quinases / Inibidores de Proteínas Quinases Limite: Animals / Humans Idioma: En Revista: J Med Chem Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Encéfalo / Desenho de Fármacos / Proteínas tau / Proteínas Serina-Treonina Quinases / Inibidores de Proteínas Quinases Limite: Animals / Humans Idioma: En Revista: J Med Chem Ano de publicação: 2021 Tipo de documento: Article