期刊
CHEMISTRY-AN ASIAN JOURNAL
卷 15, 期 22, 页码 3836-3844出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.202001003
关键词
NOD2; Muramyl dipeptide (MDP); Peptidoglycan; Structure activity relationship; Innate immunity; Biological activity
资金
- Ministry of Science and Technology
A series of muramyl dipeptide (MDP) analogues with structural modifications at the C4 position of MurNAc and on thed-iso-glutamine (isoGln) residue of the peptide part were synthesized. The C4-diversification of MurNAc was conveniently achieved by using CuAAC click strategy to conjugate an azido muramyl dipeptide precursor with structurally diverse alkynes.d-Glutamic acid (Glu), replaced withisoGln, was applied for the structural diversity through esterification or amidation of the carboxylic acid. In total, 26 MDP analogues were synthesized and bio-evaluated for the study of human NOD2 stimulation activity in the innate immune response. Interestingly, MDP derivatives with an ester moiety are found to be more potent than reference compound MDP itself or MDP analogues containing an amide moiety. Among the varied lengths of the alkyl chain in ester derivatives, the MDP analogue bearing thed-glutamate dodecyl (C12) ester moiety showed the best NOD2 stimulation potency.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据