血脑屏障上葡萄糖转运体1研究进展  

Research progress for glucose transporter 1 at the blood brain barrier

作　　者：王玉珠[1] 刘皋林[1] 李晓宇[1] 

机构地区：[1]上海交通大学医学院附属第一人民医院药学部,上海200080

出　　处：《中国临床药理学与治疗学》2014年第9期1057-1063,共7页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：上海市自然科学基金项目(10ZR1423600);中国博士后科学基金特别资助(200902245);科技部十二五重大新药创制专项(2011ZX09302-007-02)

摘　　要：葡萄糖是中枢神经系统主要的能源物质,葡萄糖转运体（glucose transporter proteins,GLUTs）家族是哺乳动物细胞葡萄糖转运的主要载体,目前发现有13个成员。基于序列的相似性和同源性,GLUTs家族分为三类,第一类：GLUT1~GLUT4,主要运输葡萄糖;第二类：GLUT5,GLUT7,GLUT9和GLUT11,主要转运果糖;第三类：GLUT6,GLUT8,GLUT10,GLUT12和HMIT,其功能尚不清楚。其中GLUT1以异构体的形式广泛存在于多种细胞,但45 000GLUT1是介导葡萄糖跨血脑屏障的主要转运体。一些中枢神经系统疾病使GLUT1表达和功能改变,从而使糖转运过程受到干扰或糖代谢功能障碍。近来研究显示,GLUT1能介导经糖基化修饰的前体药物跨膜运输,因此,靶向于葡萄糖转运体跨血脑屏障的运载方法将会引起研究者更广泛的关注。Glucose in the central neuronal is the main energy source system. The family of facilitative glucose transporter proteins （GLUTs） is responsible for entry of glucose into brain. 13 members of the GLUTs family have been described thus far. Based on sequence similarities, the GLUTs family is divided into three classes, the first class （GLUT1-GLUT4） mostly transporting glucose~ the second class （GLUT5, GLUTT, GLUT9 and GLUT11） mainly delivering fructose; the third class（GLUT6, GLUT8, GLUT10, GLUT12 and HMIT）, however its function is still unclear. GLUT1 isomers are expressed in many kinds of cells, however,45kDa GLUT1 is the major transport protein mediating glucose across the blood brain barriers. The change of GLUT1 expression and function in some central nervous system diseases results in glucose transport process disturbed or glucose metabolism dysfunction. Recent researches show that GLUT1 can transport prodrugs by glycosylation modification across blood brain barrier. Therefore, method of glucose transport depending on GLUT1 may be a selective drug-delivery system. By utilizing such highly specific transport mechanism, it will widely attract the attention of researchers.

关 键 词：血脑屏障 GLUT1 糖基化 

分 类 号：R965[医药卫生—药理学]