Development, optimization, and in vivo validation of new imidazopyridine chemotypes as dual TLR7/TLR9 antagonists through activity-directed sequential …
Undesirable activation of endosomal toll-like receptors TLR7 and TLR9 present in specific
immune cells in response to host-derived ligands is implicated in several autoimmune …
immune cells in response to host-derived ligands is implicated in several autoimmune …
Systematic optimization of potent and orally bioavailable purine scaffold as a dual inhibitor of toll-like receptors 7 and 9
Several toll-like receptors (TLRs) reside inside endosomes of specific immune cells—among
them, aberrant activation of TLR7 and TLR9 is implicated in myriad contexts of autoimmune …
them, aberrant activation of TLR7 and TLR9 is implicated in myriad contexts of autoimmune …
Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8)
RK Sreekantha, CP Mussari, DS Dodd… - ACS Medicinal …, 2022 - ACS Publications
The toll-like receptors (TLRs) play key roles in activation of the innate immune system.
Aberrant activation of TLR7 and TLR8 pathways can occur in the context of autoimmune …
Aberrant activation of TLR7 and TLR8 pathways can occur in the context of autoimmune …
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 …
T Knoepfel, P Nimsgern, S Jacquier… - Journal of medicinal …, 2020 - ACS Publications
Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune
diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a …
diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a …
Activity-guided development of potent and selective toll-like receptor 9 antagonists
TLR9 is one of the major innate immune receptors expressed in the endosomes of pDCs
and B cells in humans. Aberrant TLR9 activation is implicated in several autoimmune and …
and B cells in humans. Aberrant TLR9 activation is implicated in several autoimmune and …
Discovery of potent and orally bioavailable small molecule antagonists of Toll-like receptors 7/8/9 (TLR7/8/9)
CP Mussari, DS Dodd, RK Sreekantha… - ACS Medicinal …, 2020 - ACS Publications
The toll-like receptor (TLR) family is an evolutionarily conserved component of the innate
immune system, responsible for the early detection of foreign or endogenous threat signals …
immune system, responsible for the early detection of foreign or endogenous threat signals …
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway
PB Alper, J Deane, C Betschart, D Buffet… - Bioorganic & Medicinal …, 2020 - Elsevier
Antagonism of the Toll-like receptors (TLRs) 7 and TLR8 has been hypothesized to be
beneficial to patients suffering from autoimmune conditions. A phenotypic screen for small …
beneficial to patients suffering from autoimmune conditions. A phenotypic screen for small …
Discovery of novel small molecule dual inhibitors targeting Toll-like receptors 7 and 8
R Padilla-Salinas, R Anderson… - Journal of Medicinal …, 2019 - ACS Publications
Endosomal toll-like receptors (TLRs) 7 and 8 recognize viral single-stranded RNAs, a class
of imidazoquinoline compounds, 8-oxo-adenosines, 8-aminobenzodiazepines, pyrimidines …
of imidazoquinoline compounds, 8-oxo-adenosines, 8-aminobenzodiazepines, pyrimidines …
Recent trends in the development of Toll-like receptor 7/8-targeting therapeutics
X Huang, X Zhang, M Lu - Expert Opinion on Drug Discovery, 2021 - Taylor & Francis
Introduction: Toll-like receptor (TLR) 7 and TLR8 are functionally localized to endosomes
and recognize specific RNA sequences. They play crucial roles in initiating innate and …
and recognize specific RNA sequences. They play crucial roles in initiating innate and …
A chemical switch for transforming a purine agonist for toll-like receptor 7 to a clinically relevant antagonist
A Mukherjee, D Raychaudhuri, BP Sinha… - Journal of Medicinal …, 2020 - ACS Publications
Toll-like receptor 7 (TLR7) is an established therapeutic target in myriad autoimmune
disorders, but no TLR7 antagonist is available for clinical use to date. Herein, we report a …
disorders, but no TLR7 antagonist is available for clinical use to date. Herein, we report a …