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 …

TLR2 agonistic small molecules: detailed structure–activity relationship, applications, and future prospects

A Kaur, D Kaushik, S Piplani, SK Mehta… - Journal of Medicinal …, 2020 - ACS Publications
Toll-like receptors (TLRs) are the pattern recognition receptors (PRRs) that recognize
pathogen-associated molecular patterns (PAMPs) in microbial species. Among the various …

Guiding principles in the design of molecular bioconjugates for vaccine applications

H Liu, DJ Irvine - Bioconjugate chemistry, 2015 - ACS Publications
Antigen-and adjuvant-based bioconjugates that can stimulate the immune system play an
important role in vaccine applications. Bioconjugates have demonstrated unique …

Determinants of activity at human Toll-like receptors 7 and 8: quantitative structure–activity relationship (QSAR) of diverse heterocyclic scaffolds

E Yoo, DB Salunke, D Sil, X Guo… - Journal of medicinal …, 2014 - ACS Publications
Toll-like receptor (TLR) 7 and 8 agonists are potential vaccine adjuvants, since they directly
activate APCs and enhance Th1-driven immune responses. Previous SAR investigations in …

Therapeutic cyclic lipopeptides mining from microbes: latest strides and hurdles

S Patel, S Ahmed, JS Eswari - World Journal of Microbiology and …, 2015 - Springer
Infectious diseases impose serious public health burdens and often have devastating
consequences. The cyclic lipopeptides elaborated by bacteria Bacillus, Paenibacillus …

Structure-based design of human TLR8-specific agonists with augmented potency and adjuvanticity

M Beesu, G Caruso, ACD Salyer… - Journal of medicinal …, 2015 - ACS Publications
Human Toll-like receptor 8 (hTLR8) is expressed in myeloid dendritic cells, monocytes, and
monocyte-derived dendritic cells. Engagement by TLR8 agonists evokes a distinct cytokine …

Identification of adjuvantic activity of amphotericin B in a novel, multiplexed, poly-TLR/NLR high-throughput screen

ACD Salyer, G Caruso, KK Khetani, LM Fox… - PLoS …, 2016 - journals.plos.org
Small-molecule agonists have been identified for TLR7, TLR8, TLR4 and TLR2 thus far, and
chemotypes other than those of canonical ligands are yet to be explored for a number of …

Diprovocims: a new and exceptionally potent class of toll-like receptor agonists

MD Morin, Y Wang, BT Jones, Y Mifune… - Journal of the …, 2018 - ACS Publications
A screen conducted with nearly 100000 compounds and a surrogate functional assay for
stimulation of an immune response that measured the release of TNF-α from treated human …

Site-specific incorporation of three toll-like receptor 2 targeting adjuvants into semisynthetic, molecularly defined nanoparticles: application to group a streptococcal …

PM Moyle, W Dai, Y Zhang, MR Batzloff… - Bioconjugate …, 2014 - ACS Publications
Subunit vaccines offer a means to produce safer, more defined vaccines compared to
traditional whole microorganism approaches. Subunit antigens, however, exhibit weak …

Identification of high-potency human TLR8 and dual TLR7/TLR8 agonists in pyrimidine-2, 4-diamines

M Beesu, ACD Salyer, MJH Brush… - Journal of medicinal …, 2017 - ACS Publications
The induction of toll-like receptor 7 (TLR7)-dependent type I interferons (IFN-α/β) from
plasmacytoid dendritic cells as well as the production of TLR8-dependent type II interferon …