Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases.


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:
10 Aug 2023
Historique:
received: 13 04 2023
accepted: 30 06 2023
pmc-release: 10 08 2024
medline: 16 8 2023
pubmed: 16 8 2023
entrez: 16 8 2023
Statut: epublish

Résumé

Toll-like receptor (TLR) 7 and TLR8 are endosomal sensors of the innate immune system that are activated by GU-rich single stranded RNA (ssRNA). Multiple genetic and functional lines of evidence link chronic activation of TLR7/8 to the pathogenesis of systemic autoimmune diseases (sAID) such as Sjögren's syndrome (SjS) and systemic lupus erythematosus (SLE). This makes targeting TLR7/8-induced inflammation with small-molecule inhibitors an attractive approach for the treatment of patients suffering from systemic autoimmune diseases. Here, we describe how structure-based optimization of compound

Identifiants

pubmed: 37583811
doi: 10.1021/acsmedchemlett.3c00136
pmc: PMC10424326
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1054-1062

Informations de copyright

© 2023 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Phil Alper (P)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Claudia Betschart (C)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Cédric André (C)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Thomas Boulay (T)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Dai Cheng (D)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Jonathan Deane (J)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Michael Faller (M)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Roland Feifel (R)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Ralf Glatthar (R)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Dong Han (D)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Rene Hemmig (R)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Tao Jiang (T)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Thomas Knoepfel (T)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Jillian Maginnis (J)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Daniel Mutnick (D)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Wei Pei (W)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Giulia Ruzzante (G)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Peter Syka (P)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Guobao Zhang (G)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Yi Zhang (Y)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Florence Zink (F)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Géraldine Zipfel (G)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Stuart Hawtin (S)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Tobias Junt (T)

Novartis Institutes for Biomedical Research, Fabrikstrasse 2, Novartis Campus, CH-4056 Basel, Switzerland.

Pierre-Yves Michellys (PY)

Novartis Institutes for Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Classifications MeSH