Modulation of the innate immune response by targeting toll-like receptors: a perspective on their agonists and antagonists

S Federico, L Pozzetti, A Papa, G Carullo… - Journal of Medicinal …, 2020 - ACS Publications
Toll-like receptors (TLRs) are a class of proteins that recognize pathogen-associated
molecular patterns (PAMPs) and damaged-associated molecular patterns (DAMPs), and …

Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles

D Kaushik, A Kaur, N Petrovsky… - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Several synthetic heterocyclic small molecules like imiquimod, resiquimod, CL097, CL075,
bromopirone, tilorone, loxoribine and isatoribine demonstrated TLR7/8 agonistic activity and …

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 …

Structural evolution and translational potential for agonists and antagonists of endosomal toll-like receptors

A Talukdar, D Ganguly, S Roy, N Das… - Journal of Medicinal …, 2021 - ACS Publications
Toll-like receptors (TLRs) are members of a large family of evolutionarily conserved pattern
recognition receptors (PRRs), which serve as key components of the innate immune system …

Novel and Selective TLR7 Antagonists among the Imidazo[1,2-a]pyrazines, Imidazo[1,5-a]quinoxalines, and Pyrazolo[1,5-a]quinoxalines Series

N Bou Karroum, G Moarbess, JF Guichou… - Journal of Medicinal …, 2019 - ACS Publications
The Toll-like receptors (TLRs) 7 and 8 play an important role in the immune system
activation, and their agonists may therefore serve as promising candidate vaccine adjuvants …

Synthesis and Optimization of 1-Substituted Imidazo[4,5-c]quinoline TLR7 Agonists

EG DeYoung, JM Howe, S Fang… - ACS Medicinal …, 2023 - ACS Publications
TLR7 agonists have significant therapeutic potential in a variety of oncology and
autoimmune applications. We recently reported a potent TLR7 selective agonist 1 that could …

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 …

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 …

Design, Synthesis, and Biological Evaluation of New 2, 6, 7-Substituted Purine Derivatives as Toll-like Receptor 7 Agonists for Intranasal Vaccine Adjuvants

M Kim, K Noh, P Kim, JH Kim, BW Choi… - Journal of Medicinal …, 2024 - ACS Publications
TLR7/8 agonists are versatile immune stimulators capable of treating various diseases such
as viral infections, autoimmune, and cancer. Despite the structural similarity of TLR7/8, their …

The novel selective TLR7 agonist GY101 suppresses colon cancer growth by stimulating immune cells

S Ren, J Chang, R Liu, G Jin - European Journal of Pharmacology, 2024 - Elsevier
Abstract Toll-like receptor (TLR) 7, a transmembrane signal transduction receptor expressed
on the surface of endosomes, has become an attractive target for antiviral and cancer …