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 …

Latest advances in small molecule TLR 7/8 agonist drug research

DC McGowan - Current Topics in Medicinal Chemistry, 2019 - ingentaconnect.com
Toll-like receptors (TLRs) 7 and 8 play an important role in the activation of innate immune
cells in mammals. These evolutionarily conserved receptors serve as important sentinels in …

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 …

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 …

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 …

Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology

L He, MY Zhang, M Cox, Q Zhang… - ACS Medicinal …, 2024 - ACS Publications
Small molecule toll-like receptor (TLR) 7 agonists have gathered considerable interest as
promising therapeutic agents for applications in cancer immunotherapy. Herein, we describe …

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 …

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 …

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 …

Structural Optimization and Biological Evaluation of Isoxazolo[5,4-d]pyrimidines as Selective Toll-Like Receptor 7 Agonists

N Strašek Benedik, A Dolšak, U Švajger… - ACS …, 2024 - ACS Publications
Toll-like receptors (TLRs) are components of innate immunity that play a crucial role in
several diseases, including chronic inflammatory and infectious diseases, autoimmune …