靶向NQO1抗肿瘤醌构效关系研究进展(英文)  

Advances on structure-activity relationship ofNQO1-targeting antitumor quinones

作　　者：廖珂[1] 牛芳[1] 郝海平[1] 王广基[1] 

机构地区：[1]中国药科大学药物代谢动力学重点实验室"天然药物活性组分与药效"国家重点实验室,南京210009

出　　处：《中国天然药物》2012年第3期170-176,共7页

基　　金：supported by the Special Fund for the Author of National Excellent Doctoral Dissertation of China (No.200979)~~

摘　　要：NAD(P)H:醌氧化还原酶1(NQO1)专性催化醌两电子还原反应, 具有化学保护和生物激活作用。NQO1 在多种肿瘤细胞特别是肺癌、结肠癌、乳腺癌细胞中的表达远高于正常组织。由于NQO1在肿瘤细胞的高表达及其生物活化的特性, 它被认为是治疗多种肿瘤的潜在分子靶标。靶向 NQO1 药物有望实现高选择性、特异性杀灭肿瘤细胞。本文重点综述了该类化合物构效关系研究, 并提出了新的研究思路, 旨在促进对靶向 NQO1 抗肿瘤醌的研究和开发。NAD（P）H：quinone oxidoreductase 1（NQO1） is an obligate two-electron reductase that is involved in chemoprotectionand can also bioactivate certain antitumor quinones.Levels of NQO1 expression are elevated in tumors particularly in those of thelung,colon and breast in relation to the surrounding normal tissues.The high levels of NQO1 in solid tumors in combination with theability to reduce many quinone-containing antitumor drugs has drawn our attention to NQO1 as a potential molecular target in cancertreatment.NQO1-targeting drugs are thus expected to achieve high selectivity and specificity to kill tumor cells.This review focuses ondiscussing the structure-activity relationships of NQO1-targeting antitumor quinones,from which possible future prospectives in thisarea are presented,in order to ignite and promote the development of NQO1-targeting antitumor drugs.

关 键 词：NAD(P)H:醌氧化还原酶1 构效关系 抗肿瘤醌 

分 类 号：R965[医药卫生—药理学]