Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
11 Jun 2020
Historique:
received: 03 03 2020
accepted: 27 04 2020
entrez: 20 6 2020
pubmed: 20 6 2020
medline: 20 6 2020
Statut: epublish

Résumé

γ-Secretase (GS) is a key target for the potential treatment of Alzheimer's disease. While inhibiting GS led to serious side effects, its modulation holds a lot of potential to deliver a safe treatment. Herein, we report the discovery of a potent and selective gamma secretase modulator (GSM) (

Identifiants

pubmed: 32551009
doi: 10.1021/acsmedchemlett.0c00109
pmc: PMC7294721
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1257-1268

Informations de copyright

Copyright © 2020 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Hasane Ratni (H)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Andre Alker (A)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Bjoern Bartels (B)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Caterina Bissantz (C)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Weichun Chen (W)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Shanghai, Cai Lun Road 720, 201203 Shanghai, China.

Irene Gerlach (I)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Anja Limberg (A)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Mingqiu Lu (M)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Shanghai, Cai Lun Road 720, 201203 Shanghai, China.

Werner Neidhart (W)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Solen Pichereau (S)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Michael Reutlinger (M)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Rosa-Maria Rodriguez-Sarmiento (RM)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Roland Jakob-Roetne (R)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Georg Schmitt (G)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Eric Zhang (E)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Shanghai, Cai Lun Road 720, 201203 Shanghai, China.

Karlheinz Baumann (K)

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

Classifications MeSH