Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay

Thomas Knoepfel,Pierre Nimsgern,Sébastien Jacquier,Marjorie Bourrel,Eric Vangrevelinghe,Ralf Glatthar,Dirk Behnke,Phil B. Alper,Pierre-Yves Michellys,Jonathan A. Deane,Tobias Junt,Géraldine Collignon Zipfel,Sarah Limonta,Stuart Hawtin,Cédric André,Thomas Boulay,Pius Loetscher,Michael Faller,Jutta Blank,Roland Feifel,Claudia Betschart

Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay

2020

Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a TLR8 antagonist competition...

Keywords:

Pharmacology
Chemistry
Endosome
Toll-like receptor
systemic lupus
Antagonist
TLR8
TLR7

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