Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.

Alzheimer Disease / metabolism Amyloid Precursor Protein Secretases / antagonists & inhibitors Animals Aspartic Acid Endopeptidases / antagonists & inhibitors Cell Line Dogs Dose-Response Relationship, Drug Drug Discovery Enzyme Inhibitors / chemical synthesis Humans Male Mice Mice, Inbred C57BL Molecular Structure Oxazines / chemical synthesis Rats Rats, Sprague-Dawley Structure-Activity Relationship

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:
28 10 2021
Historique:
pubmed: 15 10 2021
medline: 15 12 2021
entrez: 14 10 2021
Statut: ppublish

Résumé

After identification of lead compound

Identifiants

DOI: 10.1021/acs.jmedchem.1c01300 PMID: 34648711
pubmed: 34648711
doi: 10.1021/acs.jmedchem.1c01300
doi:

Substances chimiques

Enzyme Inhibitors 0
Oxazines 0
Umibecestat 4612B80545
Amyloid Precursor Protein Secretases EC 3.4.-
Aspartic Acid Endopeptidases EC 3.4.23.-
BACE1 protein, human EC 3.4.23.46

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

15262-15279

Auteurs

Rainer Machauer (R)

Global Discovery Chemistry, Novartis Pharma AG, CH-4056 Basel, Switzerland.
ORCID: 0000-0001-5081-6268

Rainer Lueoend (R)

Global Discovery Chemistry, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Konstanze Hurth (K)

Global Discovery Chemistry, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Siem J Veenstra (SJ)

Global Discovery Chemistry, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Heinrich Rueeger (H)

Global Discovery Chemistry, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Markus Voegtle (M)

Global Discovery Chemistry, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Marina Tintelnot-Blomley (M)

Global Discovery Chemistry, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Jean-Michel Rondeau (JM)

Chemical Biology and Therapeutics, Structural Biology Platform, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Laura H Jacobson (LH)

Department of Neuroscience, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Grit Laue (G)

Pharmacokinetic-Sciences, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Karen Beltz (K)

Pharmacokinetic-Sciences, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Ulf Neumann (U)

Department of Neuroscience, Novartis Pharma AG, CH-4056 Basel, Switzerland.

Articles similaires

[Redispensing of expensive oral anticancer medicines: a practical application].

Lisanne N van Merendonk, Kübra Akgöl, Bastiaan Nuijen
1.00
Humans Antineoplastic Agents Administration, Oral Drug Costs Counterfeit Drugs

Smoking Cessation and Incident Cardiovascular Disease.

Jun Hwan Cho, Seung Yong Shin, Hoseob Kim et al.
1.00
Humans Male Smoking Cessation Cardiovascular Diseases Female

Evaluation of Low-Value Services Across Major Medicare Advantage Insurers and Traditional Medicare.

Ciara Duggan, Adam L Beckman, Ishani Ganguli et al.
1.00
Humans United States Aged Cross-Sectional Studies Medicare Part C

Effectiveness of Virtual Yoga for Chronic Low Back Pain: A Randomized Clinical Trial.

Hallie Tankha, Devyn Gaskins, Amanda Shallcross et al.
1.00
Humans Yoga Low Back Pain Female Male

Classifications MeSH

questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Peptide hydrolases › Endopeptidases › Amyloid precursor protein secretases › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Eucaryotes › Animaux › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Peptide hydrolases › Endopeptidases › Aspartic acid endopeptidases › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Cellules › Cellules cultivées › Lignée cellulaire › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Carnivora › Pinnipedia › Canidae › Chiens › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée C57BL › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Oxazines › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Rat Sprague-Dawley › Discovery of Umibecestat (CNP520): A Potent,...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery of Umibecestat (CNP520): A Potent,...