氨基酸修饰的α-GalCer 类似物的合成与评价。
Synthesis and evaluation of amino-modified alpha-GalCer analogues.
机构信息
Laboratory for Medicinal Chemistry (FFW), Ghent University, Harelbekestraat 72, 9000 Ghent, Belgium.
出版信息
Org Lett. 2010 Jul 2;12(13):2928-31. doi: 10.1021/ol100934z.
Abstract
Alpha-GalCer analogues featuring a phytoceramide 3- and 4-amino group have been synthesized. A Mitsunobu reaction involving phthalimide was employed for the introduction of the amino groups at the 3- and 4-positions of suitable phytosphingosine-derived precursors. The influence of these modifications on the interaction with the T-cell receptor of NKT cells was investigated, as well as the capacity of the amino-modified analogues to induce a cytokine response after in vivo administration.
摘要
已经合成了具有植物神经酰胺 3- 和 4-氨基基团的 α-GalCer 类似物。采用 Mitsunobu 反应引入邻苯二甲酰亚胺，将氨基基团引入合适的植物神经鞘氨醇衍生前体的 3-和 4-位。研究了这些修饰对与 NKT 细胞 T 细胞受体相互作用的影响，以及在体内给药后，氨基修饰类似物诱导细胞因子反应的能力。
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