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 …

Recent advances in hepatitis B treatment

GM Prifti, D Moianos, E Giannakopoulou, V Pardali… - Pharmaceuticals, 2021 - mdpi.com
Hepatitis B virus infection affects over 250 million chronic carriers, causing more than
800,000 deaths annually, although a safe and effective vaccine is available. Currently used …

Design, synthesis, crystal structure, and antimicrobial evaluation of 6-fluoroquinazolinylpiperidinyl-containing 1, 2, 4-triazole Mannich base derivatives against …

J Shi, M Ding, N Luo, S Wan, P Li, J Li… - Journal of Agricultural …, 2020 - ACS Publications
A total of 20 1, 2, 4-triazole Mannich base derivatives bearing the 6-
fluoroquinazolinylpiperidinyl moiety were designed, synthesized, and evaluated as …

Discovery of GS-9688 (Selgantolimod) as a potent and selective oral toll-like receptor 8 agonist for the treatment of chronic hepatitis B

RL Mackman, M Mish, G Chin, JK Perry… - Journal of Medicinal …, 2020 - ACS Publications
Toll-like receptor 8 (TLR8) recognizes pathogen-derived single-stranded RNA fragments to
trigger innate and adaptive immune responses. Chronic hepatitis B (CHB) is associated with …

A 1, 2, 3-Triazole derivative of quinazoline exhibits antitumor activity by tethering RNF168 to SQSTM1/P62

FC Wang, B Peng, TT Ren, SP Liu, JR Du… - Journal of Medicinal …, 2022 - ACS Publications
Quinazoline and its derivatives have drawn much attention in the development of potential
antitumor agents. Here, we synthesized a series of 1, 2, 3-triazole derivatives of quinazoline …

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 …

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 …

Toll-like receptors 7/8: a paradigm for the manipulation of immunologic reactions for immunotherapy

F Li, B Song, WF Zhou, LJ Chu - Viral Immunology, 2023 - liebertpub.com
The innate immune system recognizes conserved features of viral and microbial pathogens
through pattern recognition receptors (PRRs). Toll-like receptors (TLR s) are one type of …

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 …