Small-molecule inhibition of TLR8 through stabilization of its resting state

S Zhang, Z Hu, H Tanji, S Jiang, N Das, J Li… - Nature chemical …, 2018 - nature.com
Endosomal Toll-like receptors (TLR3, TLR7, TLR8, and TLR9) are highly analogous sensors
for various viral or bacterial RNA and DNA molecular patterns. Nonetheless, few small …

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 …

Structural reorganization of the Toll-like receptor 8 dimer induced by agonistic ligands

H Tanji, U Ohto, T Shibata, K Miyake, T Shimizu - Science, 2013 - science.org
Toll-like receptor 7 (TLR7) and TLR8 recognize single-stranded RNA and initiate innate
immune responses. Several synthetic agonists of TLR7-TLR8 display novel therapeutic …

Small-molecule TLR8 antagonists via structure-based rational design

Z Hu, H Tanji, S Jiang, S Zhang, K Koo, J Chan… - Cell chemical …, 2018 - cell.com
Rational design of drug-like small-molecule ligands based on structural information of
proteins remains a significant challenge in chemical biology. In particular, designs targeting …

Recent advances on small-molecule antagonists targeting TLR7

H Zheng, P Wu, PA Bonnet - Molecules, 2023 - mdpi.com
Toll-like receptor 7 (TLR7) is a class of pattern recognition receptors (PRRs) recognizing the
pathogen-associated elements and damage and as such is a major player in the innate …

A five-amino-acid motif in the undefined region of the TLR8 ectodomain is required for species-specific ligand recognition

J Liu, C Xu, LC Hsu, Y Luo, R Xiang, TH Chuang - Molecular immunology, 2010 - Elsevier
Toll-like receptors play important roles in regulating immunity against microbial infections.
Toll-like receptor 8 (TLR8) belongs to a subfamily comprising TLR7, TLR8 and TLR9 …

Structural analyses of toll-like receptor 7 reveal detailed RNA sequence specificity and recognition mechanism of agonistic ligands

Z Zhang, U Ohto, T Shibata, M Taoka, Y Yamauchi… - Cell reports, 2018 - cell.com
Summary Toll-like receptor 7 (TLR7) is an innate immune receptor for single-stranded RNA
(ssRNA) and has important roles in infectious diseases. We previously reported that TLR7 …

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 …

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 …

Toll-like receptor 4 (TLR4) inhibitors: Current research and prospective

Y Zhang, X Liang, X Bao, W Xiao, G Chen - European journal of medicinal …, 2022 - Elsevier
Abstract Toll-like receptor 4 (TLR4), a member of the Toll-like receptor (TLR) family, is
involved in innate immunity and mediates inflammatory responses by recognizing …