Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.

Animals Brain / metabolism Drug Design Humans Indazoles / chemistry Mice Molecular Targeted Therapy Phosphorylation / drug effects Protein Kinase Inhibitors / chemistry Protein Serine-Threonine Kinases / antagonists & inhibitors Rats tau Proteins / metabolism

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
13 05 2021
Historique:
pubmed: 5 5 2021
medline: 16 6 2021
entrez: 4 5 2021
Statut: ppublish

Résumé

Structural analysis of the known NIK inhibitor

Identifiants

DOI: 10.1021/acs.jmedchem.1c00382 PMID: 33944571
pubmed: 33944571
doi: 10.1021/acs.jmedchem.1c00382
doi:

Substances chimiques

Indazoles 0
Protein Kinase Inhibitors 0
tau Proteins 0
tau-tubulin kinase EC 2.7.1.11
Protein Serine-Threonine Kinases EC 2.7.11.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

6358-6380

Auteurs

Tamara Halkina (T)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Jaclyn L Henderson (JL)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
ORCID: 0000-0002-7097-1350

Edward Y Lin (EY)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Martin K Himmelbauer (MK)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
ORCID: 0000-0003-4960-4457

J Howard Jones (JH)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Marta Nevalainen (M)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Jun Feng (J)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Kristopher King (K)

Department of Drug Metabolism and Pharmacokinetics, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Michael Rooney (M)

Department of Drug Metabolism and Pharmacokinetics, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Joshua L Johnson (JL)

Department of Drug Metabolism and Pharmacokinetics, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Douglas J Marcotte (DJ)

Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Jayanth V Chodaparambil (JV)

Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

P Rajesh Kumar (PR)

Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Thomas A Patterson (TA)

Department of Physical Biochemistry and Molecular Design, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Paramasivam Murugan (P)

Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Eli Schuman (E)

Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

LaiYee Wong (L)

Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Thomas Hesson (T)

Department of Bioassays, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Sarah Lamore (S)

Department of Preclinical Safety, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Channa Bao (C)

Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Michael Calhoun (M)

Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Hannah Certo (H)

Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Brenda Amaral (B)

Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Gregory M Dillon (GM)

Department of Emerging Neurosciences Research Unit, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Rab Gilfillan (R)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Felix Gonzalez-Lopez de Turiso (FG)

Department of Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
ORCID: 0000-0001-9736-0907

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Indazoles › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Thérapeutique › Traitement médicamenteux › Thérapie moléculaire ciblée › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Métabolisme › Phosphorylation › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Protein-Serine-Threonine Kinases › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery of Potent and Brain-Penetrant Tau...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines de tissu nerveux › Protéines associées aux microtubules › Protéines tau › Discovery of Potent and Brain-Penetrant Tau...