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Agonists of Toll-like Receptor 2 (TLR2) are attractive synthetic targets due to their use as adjuvants in immunotherapies to treat various diseases notably, cancer. An indepth understanding of TLR2 agonist structure-activity relationships is therefore advantageous for the methodical design of vaccines targetting the TLR2 machinery. This review aims to collate and discuss the literature regarding synthetic studies towards TLR2 agonists and the structure-activity relationships thereof. It is hoped that interested readers will gain a holistic understanding of this topic, and will prompt further efforts towards finding effective agonists of TLR2.
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http://dx.doi.org/10.1039/d0ob00942c | DOI Listing |
Spectrochim Acta A Mol Biomol Spectrosc
September 2025
College of Chemistry, Zhengzhou University, Zhengzhou, Henan 450001, PR China.
The interactions of three berberine mid-chain fatty acid salts ([BBR][C], n = 6, 7, 8) with lysozyme (Lyz) are investigated in detail using multi-spectroscopic and molecular docking techniques. Steady-state fluorescence and UV-visible absorption experiments suggest that the binding mechanism of [BBR][C] on Lyz is a static quenching with a binding ratio of 1:1. The compound [BBR][C] exhibits a moderate binding affinity toward Lyz.
View Article and Find Full Text PDFChem Biodivers
September 2025
Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Molecular, Structural and Translational Virology Research Group, KU Leuven, Leuven, Belgium.
The human chemokine receptor 8 (CCR8) received attention as target for the treatment of various autoimmune disorders. Phenoxybenzylpiperidine analogues are known to act as CCR8 agonists, although their structure-activity relationship (SAR) has been studied to a limited extent. In this study, the SAR of phenoxybenzylpiperidinyl analogues was explored in a systematic way by fusion or insertion of various heterocyclic groups on the piperidinyl ring, yielding a set of 21 novel phenoxybenzylpiperidinyl derivatives.
View Article and Find Full Text PDFChem Biodivers
September 2025
Key Lab of Natural Product Chemistry and Application at Universities of Education, Department of Xinjiang Uygur Autonomous Region, School of Chemistry and Chemical Engineering, Yili Normal University, Xinjiang, China.
The persistent threat posed by phytopathogenic fungi to agricultural systems underscores the critical need for novel fungicides. Here, we synthesized and characterized a series of novel acridospiroisoxazole derivatives (H1-H36) using H/C NMR and mass spectrometry. The absolute configuration of compound H23 was confirmed using single-crystal x-ray diffraction analysis.
View Article and Find Full Text PDFACS Chem Neurosci
September 2025
Department of Medical Biology, Faculty of Medicine, Bahçeşehir University, Istanbul 34353, Turkey.
IL-17A is a pro-inflammatory cytokine that significantly contributes to the pathogenesis of autoimmune diseases, including multiple sclerosis (MS). Previous studies have suggested that PARP-1 inhibitors can modulate IL-17A-mediated inflammation, prompting the investigation of Niraparib, an FDA-approved PARP-1 inhibitor, as a potential therapeutic agent for MS. In this study, we hypothesized that Niraparib could disrupt the interaction between IL-17A and its receptor, IL-17RA.
View Article and Find Full Text PDFChemMedChem
September 2025
Institute of Organic Chemistry, Leipzig University, Johannisallee 29, 04103, Leipzig, Germany.
The transcription factor signal transducer and activator of transcription (STAT)4 is a potential target for autoimmune diseases, such as inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes mellitus. p-Biphenyl phosphate is reported as an inhibitor of the STAT4 Src homology 2 domain, and it is developed to the phosphonate-based inhibitor Stafori-1. Herein, structure-activity relationships of p-biaryl phosphates against STAT4 and their selectivity profiles against other STAT proteins are reported.
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