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新型C型凝集素受体Mincle激动剂12-单糖基和二糖基氧化硬脂酸酯的合成

Synthesis of 12--Mono- and Diglycosyl-oxystearates, a New Class of Agonists for the C-type Lectin Receptor Mincle.

作者信息

Van Huy Le, Tanaka Chiaki, Imai Takashi, Yamasaki Sho, Miyamoto Tomofumi

机构信息

Department of Natural Products Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka 812-8582, Japan.

Department of Molecular Immunology, Immunology Frontier Research Center, Osaka University, Osaka 565-0871, Japan.

出版信息

ACS Med Chem Lett. 2018 Dec 13;10(1):44-49. doi: 10.1021/acsmedchemlett.8b00413. eCollection 2019 Jan 10.

Abstract

Fifteen glycosyl-oxystearates were synthesized by Crich's 4,6-benzylidene and Köening-Knorr strategies. Assessment of structure-activity relationships using macrophage-inducible C-type lectin (Mincle) receptor cells expressing nuclear factor of activated T cells (NFAT)-green fluorescent protein (GFP) revealed that four dimannopyranosyl-oxystearate analogues were Mincle agonists and that 12--(2--α-d-mannopyranosyl)-α-d-mannopyranosyl-oxystearate was as an activator of both mouse and human Mincle.

摘要

通过克里奇(Crich)的4,6-亚苄基策略和柯宁-克诺尔(Köening-Knorr)策略合成了15种糖基-氧代硬脂酸酯。使用表达活化T细胞核因子(NFAT)-绿色荧光蛋白(GFP)的巨噬细胞诱导型C型凝集素(Mincle)受体细胞评估构效关系,结果显示四种二甘露吡喃糖基-氧代硬脂酸酯类似物是Mincle激动剂,并且12-(2-α-d-甘露吡喃糖基)-α-d-甘露吡喃糖基-氧代硬脂酸酯是小鼠和人Mincle的激活剂。

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本文引用的文献

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Sensing Lipids with Mincle: Structure and Function.用巨噬细胞C型凝集素(Mincle)感知脂质:结构与功能
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