Structure modifications based on KRN7000 and their SARs in activating NKT cells  

基于KRN7000的结构改造以及它们对自然杀伤T细胞活化作用的构效关系(英文)

作　　者：张蕾[1] 叶新山[1] 

机构地区：[1]北京大学 天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2008年第4期263-271,共9页中国药学（英文版）

基　　金：National Natural Science Foundation of China (Grant No.90713010);"863"Program from the Ministry of Science and Technology of China (Grant No.2006AA09Z405).

摘　　要：α-Galactosylceramides, which can be recognized by natural killer T （NKT） cells, are now attracting more and more attention due to their therapeutic potential in cancer, infection and autoimmune diseases. Advances have been achieved in discovering compounds with better activities and efforts have been made to understand the structure-activity relationships （SARs） of these NKT cell ligands. In this review, we discuss the structure modifications based on KRN7000, the principal glycolipid used in the study of NKT cell stimulation, and the SARs based on these modified structures.能够被自然杀伤T细胞所识别的α-半乳糖基神经酰胺具有潜在的治疗肿痛、感染性疾病和自身免疫性疾病的用途,已引起了研究者们越来越多的注意。人们在寻找具有更好活性的化合物方面取得了不少进展,在理解这些自然杀伤T细胞配体的构效关系方面进行了许多探索。KRN7000是用于自然杀伤T细胞刺激研究的一种主要的糖脂类化合物。本文对近年来基于KRN7000的各种结构改造以及在这些结构改造基础上所获得的构效关系进行详细的综述。

关 键 词：α-Galactosylceramide NKT cell activation GLYCOLIPID Immunoregulatory agent Structure-activity relationship 

分 类 号：R914[医药卫生—药物化学]