还原性叶酸载体基因多态性与甲氨蝶呤药物敏感性的相关研究进展  

The relationship between the polymorphisms of RFC and methotrexate resistance

作　　者：赵玮(综述)[1] 岳丽杰(审校)[2] 陈小文(审校)[1] 

机构地区：[1]遵义医学院珠海校区,519041 [2]深圳市儿童医院儿科研究所,518026

出　　处：《国际儿科学杂志》2010年第6期561-564,共4页International Journal of Pediatrics

基　　金：基金项目：国家自然科学基金资助项目（30471830）;深圳市科技计划项目（200802065）

摘　　要：还原性叶酸载体（RFC）是肿瘤化疗药物甲氨蝶呤（MTX）跨膜运输的主要载体,其基因多态性是造成MTX耐药的原因之一.近年来随着RFC基因多态性和功能之间关系的深入研究,人们发现RFC基因多态性引起的分子结构改变是造成MTX摄入减少的主要原因,它可以引起靶酶抑制不完全和聚谷氨酸盐形成减少,最终导致叶酸拮抗剂耐药.The best characterized methotrexate （MTX） transporter is the reduced folate carrier （RFC）,whose gene polymorphism is one of the reasons causing MTX resistance. Based on the studies in rencent years,we have known that synthesis of mutant RFC or loss of RFC transcripts and proteins results in antifolate resistance due to incomplete inhibition of cellular enzyme targets and insufficient substrate for polyglutamate synthesis. So additional human RFC structural and mechanistic studies are absolutely essential. This paper summarizes an association between the polymorphisms of RFC and MTX resistance, which can provide a basis for clinical treatment.

关 键 词：还原性叶酸载体 基因多态性 基因表达 甲氨蝶呤 药物敏感性 

分 类 号：R733.71[医药卫生—肿瘤]