...
首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Structure-activity relationship studies of Bz amide-containing alpha-GalCer derivatives as natural killer T cell modulators
【24h】

Structure-activity relationship studies of Bz amide-containing alpha-GalCer derivatives as natural killer T cell modulators

机译:BZ酰胺α-高压运动衍生物作为天然杀伤T细胞调节剂的结构 - 活性关系研究

获取原文
获取原文并翻译 | 示例
           

摘要

CD1d is a non-polymorphic antigen-presenting glycoprotein that recognizes glycolipids as ligands. Ligands bind to the hydrophobic grooves of CD1d, and the resulting ligand-CD1d complexes activate natural killer T (NKT) cells by means of T cell receptor recognition, leading to the secretion of various cytokines. However, details of the ligand recognition mechanism of a large hydrophobic ligand binding pocket and the relationship between cytokine induction and ligand structure are unclear. We report the synthesis of alpha-GalCer derivatives containing a Bz amide group having various substituting groups in the ceramide moiety, and the analysis of the structure-activity relationships. The assays reveal that the Bz amide-containing CD1d ligands function as NKT cell modulators displaying Th2 cytokine biasing responses. Furthermore, molecular dynamics simulation studies suggest that the phenyl groups can interact with the aromatic amino acid residues in the lipid binding pocket of CD1d.
机译:CD1D是一种非多态抗原呈递糖蛋白,其将糖脂作为配体识别。 配体与CD1D的疏水槽结合,并通过T细胞受体识别,得到的配体-CD1D复合物激活天然杀伤T(NKT)细胞,导致各种细胞因子的分泌。 然而,大型疏水性配体结合口袋的配体识别机制的细节和细胞因子诱导和配体结构之间的关系尚不清楚。 我们报道了含有Bz酰胺基团的α-高压运动衍生物的合成,其在神经酰胺部分中具有各种替代基团,以及结构 - 活性关系的分析。 该测定揭示了含有BZ酰胺CD1D配体的用作显示Th2细胞因子偏置反应的NKT细胞调节剂。 此外,分子动力学模拟研究表明,苯基可以与CD1D的脂质结合口袋中的芳族氨基酸残基相互作用。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号