P-65 自然免疫受容体TLR4/MD-2による認識配座解明を目指したリピドA配座固定類縁体の合成研究(ポスター発表の部)

概要

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Gram-negative bacteria have an immunostimulating glycoconjugate called LPS on its cell surface. Lipid A, the active entity of LPS, possesses two phosphate groups and several acyl chains bound to glucosamine disaccharide structure, and the reduction of the number or the length of these chains made the lipid A molecule less active or inactive. Our previous results suggested that the acyl chains are assembled by hydrophobic interaction to fix the overall conformation of lipid A molecule, and receptor of lipid A would recognize its particular conformation. In the present study, we synthesized conformationally constrained cyclic analogues of lipid A in which acyl moieties at 3 and 2' positions of glucosamine disaccharide were cross-linked by olefin metathesis. We also obtained corresponding acyclic analogues and measured the biological activities of them. One of the cyclic analogues showed potent cytokine inducing activity, whereas the corresponding acyclic analogue showed weak antagonistic activity.
天然有機化合物討論会の論文
2006-09-15