| 与CYPOR共表达CYP2D6~*1和CYP2D6~*10及其代谢活性比较 |
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| 引用本文： | 钱鸣蓉,陈静,刘瑶,余露山,陈枢青,曾苏. 与CYPOR共表达CYP2D6~*1和CYP2D6~*10及其代谢活性比较[J]. 药学学报, 2011, 0(2) |
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| 作者姓名： | 钱鸣蓉 陈静 刘瑶 余露山 陈枢青 曾苏 |
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| 作者单位： | 浙江大学药学院;浙江省农业科学院农产品质量标准研究所; |
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| 基金项目： | 国家“重大新药创制”科技重大专项课题临床前药物代谢动力学技术平台(2009ZX09304-003) |
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| 摘 要： | 细胞色素P450 2D6(cytochrome P450 2D6,CYP2D6)是一种重要的氧化代谢酶,呈基因多态性,对药物的代谢呈现明显的个体差异和种族差异,CYP2D6*10在中国人群中的发生率高达51.3%。采用杆状病毒昆虫表达系统,采用与细胞色素氧化还原酶(cytochrome oxidoreductase,CYPOR)共表达的方式获得具有代谢活性的CYP2D6*1/CYP2D6*10,并初步研究其催化右美沙芬的代谢活性差异。构建重组质粒pFastBac-CYP2D6*1,pFastBac-CYP2D6*10和pFastBac-CYPOR,并分别转化DH10Bac菌株构建重组Bacmid-CYPOR,Bacmid-CYP2D6*1和Bacmid-CYP2D6*10,转染Sf9昆虫细胞,获得重组杆状病毒用于病毒扩增和感染Sf9昆虫细胞。通过测定混悬蛋白催化右美沙芬的速率来优化重组CYPOR和CYP2D6病毒感染Sf9昆虫细胞的感染复数(multiplicity of infection,MOI)值和其比例,获得活力较高的重组CYP2D6*1和CYP2D6*10。重组CYP2D6*1催化右美沙芬的Km为(...
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| 关 键 词： | 昆虫表达系统 细胞色素P4502D6*1 细胞色素P4502D6*10 细胞色素氧化还原酶 代谢差异 |
CYP2D6~*1,CYP2D6~*10 co-expressed with CYPOR in Bac-to-Bac expression system and activity determination |
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| QIAN Ming-rong,CHEN Jing,LIU Yao,YU Lu-shan,CHEN Shu-qing,ZENG Su. CYP2D6~*1,CYP2D6~*10 co-expressed with CYPOR in Bac-to-Bac expression system and activity determination[J]. Acta pharmaceutica Sinica, 2011, 0(2) |
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| Authors: | QIAN Ming-rong CHEN Jing LIU Yao YU Lu-shan CHEN Shu-qing ZENG Su |
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| Affiliation: | QIAN Ming-rong1,2,CHEN Jing1,LIU Yao1,YU Lu-shan1,CHEN Shu-qing1,ZENG Su1(1.College of Pharmaceutical Sciences,Zhejiang University,Hangzhou 310058,China,2.Institute of Quality Standards for Agricultural Products,Zhejiang Academy of Agricultural Sciences,Hangzhou 310021,China) |
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| Abstract: | CYP2D6 is an important drug-metabolizing enzyme.The polymorphism of CYP2D6 leads to metabolism difference and the different reactions of drugs in the individuals and different races are normal phenomenon in clinical medication.CYP2D6*10 is an important subtype in Asian people and 51.3% Chinese are classified with this subtype.To obtain recombinant active CYP2D6*1/CYP2D6*10 in baculovirus system by optimizing coexpression with CYPOR,and detect their activity to catalyze dextromethorphan,three recombinants pF... |
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| Keywords: | baculovirus CYP2D6*1 CYP2D6*10 CYPOR metabolism difference |
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