Diazaspirononane Nonsaccharide Inhibitors of O-GlcNAcase (OGA) for the Treatment of Neurodegenerative Disorders.

Animals Aza Compounds / chemistry Catalysis Enzyme Inhibitors / chemistry Humans Male Mice Mice, Inbred C57BL Models, Molecular Molecular Structure Mutagenesis Neurodegenerative Diseases / drug therapy Structure-Activity Relationship beta-N-Acetylhexosaminidases / antagonists & inhibitors

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:
25 11 2020
Historique:
pubmed: 17 11 2020
medline: 22 1 2021
entrez: 16 11 2020
Statut: ppublish

Résumé

O-GlcNAcylation is a post-translational modification of tau understood to lower the speed and yield of its aggregation, a pathological hallmark of Alzheimer's disease (AD). O-GlcNAcase (OGA) is the only enzyme that removes O-linked

Identifiants

DOI: 10.1021/acs.jmedchem.0c01479 PMID: 33197187
pubmed: 33197187
doi: 10.1021/acs.jmedchem.0c01479
doi:

Substances chimiques

Aza Compounds 0
Enzyme Inhibitors 0
beta-N-Acetylhexosaminidases EC 3.2.1.52

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

14017-14044

Auteurs

Carlos M Martínez-Viturro (CM)

Discovery Chemistry, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain.
ORCID: 0000-0002-0241-6689

Andrés A Trabanco (AA)

Discovery Chemistry, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain.
ORCID: 0000-0002-4225-758X

Jordi Royes (J)

Department Química Física i Inorgànica, University Rovira i Virgili, C/Marcel·lí Domingo s/n, 43007 Tarragona, Spain.
ORCID: 0000-0001-6129-7344

Elena Fernández (E)

Department Química Física i Inorgànica, University Rovira i Virgili, C/Marcel·lí Domingo s/n, 43007 Tarragona, Spain.
ORCID: 0000-0001-9025-1791

Gary Tresadern (G)

Computational Chemistry, Janssen Research & Development, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2440 Beerse, Belgium.
ORCID: 0000-0002-4801-1644

Juan A Vega (JA)

Discovery Chemistry, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain.

Alcira Del Cerro (A)

Discovery Chemistry, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain.

Francisca Delgado (F)

Discovery Chemistry, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain.

Aránzazu García Molina (A)

Discovery Chemistry, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain.

Fulgencio Tovar (F)

Villapharma Research S.L., Parque Tecnológico de Fuente Álamo, Ctra. El Estrecho-Lobosillo, Km. 2.5-Av. Azul, 30320 Fuente Álamo de Murcia, Spain.

Paul Shaffer (P)

X-Ray Crystallography, Janssen Pharmaceutical Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477, United States.

Andreas Ebneth (A)

Neuroscience Discovery, Janssen Research & Development, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2440 Beerse, Belgium.

Alexis Bretteville (A)

Neuroscience Discovery, Janssen Research & Development, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2440 Beerse, Belgium.

Liesbeth Mertens (L)

Neuroscience Discovery, Janssen Research & Development, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2440 Beerse, Belgium.

Marijke Somers (M)

Discovery DMPK, Janssen Research & Development, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2440 Beerse, Belgium.

Jose M Alonso (JM)

Analytical Sciences, Janssen Research & Development, Janssen-Cilag, S.A., C/Jarama 75A, 45007 Toledo, Spain.

José M Bartolomé-Nebreda (JM)

Discovery Chemistry, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Composés chimiques organiques › Composés aza › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Phénomènes chimiques › Catalyse › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée C57BL › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles moléculaires › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Phénomènes génétiques › Mutagenèse › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Maladies du système nerveux › Maladies neurodégénératives › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Diazaspirononane Nonsaccharide Inhibitors of...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Glycosidases › Hexosaminidases › beta-N-Acetylhexosaminidases › Diazaspirononane Nonsaccharide Inhibitors of...