[HTML][HTML] 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 …

Small molecule agonists of toll-like receptors 7 and 8: a patent review 2014–2020

ME Kieffer, AM Patel, SA Hollingsworth… - Expert Opinion on …, 2020 - Taylor & Francis
Introduction Toll-like receptors 7 and 8 (TLR7 and TLR8) are endosomal immune receptors
that initiate an innate immune response and can facilitate activation of the adaptive immune …

[HTML][HTML] 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 …

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 …

Activity-guided development of potent and selective toll-like receptor 9 antagonists

B Paul, O Rahaman, S Roy, S Pal, S Satish… - European Journal of …, 2018 - Elsevier
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 …

Identification and characterization of a novel chemotype for human TLR8 inhibitors

D Šribar, M Grabowski, MS Murgueitio… - European journal of …, 2019 - Elsevier
The endosomal Toll-like receptor 8 (TLR8) recognizes single-stranded RNA and initiates
early inflammatory responses. Despite the importance of endosomal TLRs for human host …

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 …

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 …

Dihydropyrrolo[2,3-d]pyrimidines: Selective Toll-Like Receptor 9 Antagonists from Scaffold Morphing Efforts

M Watanabe, M Kasai, H Tomizawa… - ACS Medicinal …, 2014 - ACS Publications
Toll-like receptors (TLRs) play important roles in the innate immune system. In fact,
recognition of endogenous immune complexes containing self-nucleic acids as pathogen-or …

Systematic optimization of potent and orally bioavailable purine scaffold as a dual inhibitor of toll-like receptors 7 and 9

B Kundu, D Raychaudhuri, A Mukherjee… - Journal of Medicinal …, 2021 - ACS Publications
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 …