Synthesis and bioactivity of fluorescence- and biotin-labeled lipid A analogues for investigation of recognition mechanism in innate immunity

Fluorescence- and biotin-labeled lipid A analogues were synthesized for the investigation of bacterial lipopolysaccharide (LPS)/lipid A recognition in the innate immune system. For the introduction of the labeling moiety, a hydrophilic glutaryl-glucose linker was used for maintaining the bioactivity and also for preventing self-aggregation, which causes quenching of the fluorescence. We also observed the biological activity of the labeled compounds.