[HTML][HTML] A novel Toll-like receptor 7/8–specific antagonist E6742 ameliorates clinically relevant disease parameters in murine models of lupus

ST Ishizaka, L Hawkins, Q Chen, F Tago, T Yagi… - European Journal of …, 2023 - Elsevier
The sensing of self RNA by the endosomal Toll-like receptors (TLRs) 7 and 8 initiates
pathogenic mechanisms underlying the autoimmune disease lupus. A blockade of the …

Discovery of M5049: a novel selective toll-like receptor 7/8 inhibitor for treatment of autoimmunity

J Vlach, AT Bender, M Przetak, A Pereira… - … of Pharmacology and …, 2021 - ASPET
Toll-like receptor (TLR) 7 and TLR8 are transmembrane receptors that recognize single-
stranded RNA. Activation of these receptors results in immune cell stimulation and …

[HTML][HTML] Preclinical characterization of the Toll-like receptor 7/8 antagonist MHV370 for lupus therapy

S Hawtin, C Andre, G Collignon-Zipfel… - Cell Reports …, 2023 - cell.com
Genetic and in vivo evidence suggests that aberrant recognition of RNA-containing
autoantigens by Toll-like receptors (TLRs) 7 and 8 drives autoimmune diseases. Here we …

Oligodeoxynucleotide inhibition of Toll‐like receptors 3, 7, 8, and 9 suppresses cytokine production in a human rheumatoid arthritis model

S Sacre, A Lo, B Gregory, M Stephens… - European Journal of …, 2016 - Wiley Online Library
Toll‐like receptors (TLRs) are innate immune receptors that respond to both exogenous and
endogenous stimuli and are suggested to contribute to the perpetuation of chronic …

First‐in‐Human Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of E6742, a Dual Antagonist of Toll‐like Receptors 7 and 8, in Healthy …

N Yamakawa, F Tago, K Nakai… - Clinical …, 2023 - Wiley Online Library
The first‐in‐human phase I study for E6742, a dual toll‐like receptor (TLR) 7 and TLR8
antagonist, has been conducted to assess the safety, tolerability, and pharmacokinetics of …

Preclinical evidence for the glucocorticoid-sparing potential of a dual toll-like receptor 7/8 inhibitor in autoimmune diseases

A Deshmukh, A Pereira, N Geraci, E Tzvetkov… - … of Pharmacology and …, 2024 - ASPET
Toll-like receptor 7 (TLR7) and TLR8 are single-stranded RNA-sensing endosomal pattern
recognition receptors that evolved to defend against viral infections. However, aberrant …

Toll-like receptor 7 and TLR9 dictate autoantibody specificity and have opposing inflammatory and regulatory roles in a murine model of lupus

SR Christensen, J Shupe, K Nickerson, M Kashgarian… - Immunity, 2006 - cell.com
Antibodies (Abs) to RNA-and DNA-containing autoantigens are characteristic of systemic
lupus erythematosus (SLE). We showed previously that Toll-like receptor (TLR) 9 …

IMO-8400, a novel TLR7, TLR8 and TLR9 antagonist, inhibits disease development in lupus-prone NZBW/F1 mice (119.12)

FG Zhu, W Jiang, Y Dong, E Kandimalla… - The Journal of …, 2012 - journals.aai.org
Several studies have implicated Toll-like receptors (TLRs) 7, 8 and 9 in the development
and progression of lupus. We have developed IMO-8400, a synthetic DNA-based antagonist …

Toll-like receptors: potential targets for lupus treatment

Y Wu, W Tang, J Zuo - Acta Pharmacologica Sinica, 2015 - nature.com
Systemic lupus erythematosus (SLE) is a complex autoimmune disease characterized by the
loss of tolerance to self-nuclear antigens. Accumulating evidence shows that Toll-like …

Structural analysis reveals TLR7 dynamics underlying antagonism

S Tojo, Z Zhang, H Matsui, M Tahara, M Ikeguchi… - Nature …, 2020 - nature.com
Abstract Toll-like receptor 7 (TLR7) recognizes both microbial and endogenous RNAs and
nucleosides. Aberrant activation of TLR7 has been implicated in several autoimmune …