摘要
黄素单氧化酶(flavin-containing monooxygenases,FMOs)是仅次于细胞色素P450(cytochrome P450,CYP450)的重要Ⅰ相代谢酶,可催化含氮、硫、磷、硒等亲核杂原子的外源物及部分内源物的氧化反应。本文将介绍FMOs的生物学特征、催化机制、底物特异性、基因多态性,分析FMOs对药物代谢的影响和个体差异以及与FMOs代谢相关的疾病,为寻找新的作用靶点和设计候选药物提供理论参考。
The flavin-containing monooxygenase（FMOs） is recognized as an important complimentary enzyme system next to the cytochrome P450（CYP450）, which catalyzes the metabolism of many xenobiotics（nucleophilic heteroatom-containing chemicals） and several endobiotics. This article provides a comprehensive introduction of FMOs including the biological characteristics, catalytic mechanism, substrate specificity, genetic polymorphisms. The effect of FMOs on drug metabolism and individual differences and relation with diseases are also mentioned. It is valuable for the discovery of therapeutic targets and design of new drug candidate.
作者
杨雅坤
盛莉
李燕
YANG Ya-kun SHENG Li LI Yan(Department of Drug Metabolism, Beijing City Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Beo＇ing City Key Laboratory of Active Substances Discovery and Drug Ability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China)
出处
《药学学报》
CAS
CSCD
北大核心
2017年第10期1485-1495,共11页
Acta Pharmaceutica Sinica
基金
十二五新药创制重大专项资助项目(2012ZX09301002-001-007,2012ZX09301002-006,2012ZX09103-101-001)
关键词
黄素单氧化酶
细胞色素P450
基因多态性
个体差异
药物代谢
新药研发
flavin-containing monooxygenase
cytochrome P450
gene polymorphism
individual difference
drug metabolism
new drug development
