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寻找大鼠自然杀伤细胞激活受体NKR-P1的最佳寡糖配体。

Toward an optimal oligosaccharide ligand for rat natural killer cell activation receptor NKR-P1.

作者信息

Krist P, Herkommerová-Rajnochová E, Rauvolfová J, Semenuk T, Vavrusková P, Pavlícek J, Bezouska K, Petrus L, Kren V

机构信息

Institute of Microbiology, Laboratory of Biotransformation, Academy of Sciences of Czech Republic, Vídenská 1083, CZ-142 20, Prague 4, Czech Republic.

出版信息

Biochem Biophys Res Commun. 2001 Sep 14;287(1):11-20. doi: 10.1006/bbrc.2001.5537.

DOI:10.1006/bbrc.2001.5537
PMID:11549246
Abstract

Aminosugars have a good affinity for the NKR-P1A protein, the major activating receptor at the surface of rat natural killer cells. We have systematically investigated the structural requirements of the recombinant soluble dimeric form of the receptor for its optimal carbohydrate ligands. While N-acetylD-mannosamine was the best neutral monosaccharide ligand, its participation in the context of an extended oligosaccharide sequence was equally important. The IC(50) value for the GalNAcbeta1 --> ManNAc disaccharide was nearly 10(-10) M with a further possible increase depending on the type of the glycosidic linkage and the aglycon nature. From the point of view of its availability, stability, and affinity for the receptor and a potential in vivo use, these studies are pivotal for the design of an oligosaccharide or glycomimetics suitable for further clustering into the multivalent glycodendrimers.

摘要

氨基糖对NKR-P1A蛋白具有良好的亲和力,NKR-P1A蛋白是大鼠自然杀伤细胞表面的主要激活受体。我们系统地研究了该受体重组可溶性二聚体形式对其最佳碳水化合物配体的结构要求。虽然N-乙酰-D-甘露糖胺是最佳的中性单糖配体,但它在延长的寡糖序列中的参与同样重要。GalNAcbeta1 --> ManNAc二糖的IC(50)值接近10^(-10) M,根据糖苷键类型和糖苷配基性质,其值可能进一步增加。从其可用性、稳定性、对受体的亲和力以及体内使用潜力的角度来看,这些研究对于设计适合进一步聚合成多价糖树枝状大分子的寡糖或糖模拟物至关重要。

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