| 非水溶性药物潜在靶蛋白筛选方法探索 |
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| 引用本文： | 陶定银,夏思敏,刘晋湘,张丽华,梁振,张玉奎.非水溶性药物潜在靶蛋白筛选方法探索[J].中国科学:化学,2011(6):976-981. |
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| 作者姓名： | 陶定银 夏思敏 刘晋湘 张丽华 梁振 张玉奎 |
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| 作者单位： | 国家色谱研究分析中心中国科学院大连化学物理研究所分离分析化学重点实验室;中国科学院研究生院; |
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| 基金项目： | 国家重大科学研究计划(2007CB914100); 中国科学院知识创新工程重要方向性项目(KJCX2YW.H09)的资助 |
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| 摘 要： | 针对化学蛋白质组学在筛选非水溶性药物的靶蛋白中存在的问题,建立了以非水溶性药物颗粒为载体的靶蛋白筛选方法.通过避免药物固定化,不仅可以保留全部的药物官能团,而且减少了蛋白质在固载基质上的非特异性吸附,可提高获得数据的可信度.将非溶性药物地塞米松颗粒直接与人小细胞肺癌H446细胞提取蛋白质通过间歇性振荡孵育24h,然后采用缓冲液清洗药物颗粒,最后对药物颗粒特异性结合的蛋白质进行酶解和分离鉴定.结果表明,筛选出41个潜在的药物靶蛋白,参与了与DEX药物作用机理相关的多种蛋白质代谢通路和糖代谢通路,同时还发现部分蛋白质参与了帕金森症疾病过程.
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| 关 键 词： | 地塞米松 化学蛋白质组 药物靶蛋白 非水溶性药物 |
An exploratory method for screening candidate target proteins of insoluble drugs |
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| TAO DingYin ,XIA SiMin ,LIU JinXiang ,ZHANG LiHua ,LIANG Zhen &ZHANG YuKui Key Laboratory of Separation Science for Analytical Chemistry,National Chromatographic R.&A.Center,Dalian Institute of Chemical Physics,Chinese Academy of Sciences,Dalian ,China Graduate University of Chinese Academy of Sciences,Beijing ,China.An exploratory method for screening candidate target proteins of insoluble drugs[J].Scientia Sinica Chimica,2011(6):976-981. |
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| Authors: | TAO DingYin XIA SiMin LIU JinXiang ZHANG LiHua LIANG Zhen &ZHANG YuKui Key Laboratory of Separation Science for Analytical Chemistry National Chromatographic R&ACenter Dalian Institute of Chemical Physics Chinese Academy of Sciences Dalian China Graduate University of Chinese Academy of Sciences Beijing China |
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| Institution: | TAO DingYin 1,2,XIA SiMin 1,LIU JinXiang 1,ZHANG LiHua 1,LIANG Zhen 1 &ZHANG YuKui 1 1 Key Laboratory of Separation Science for Analytical Chemistry,National Chromatographic R.&A.Center,Dalian Institute of Chemical Physics,Chinese Academy of Sciences,Dalian 116023,China 2 Graduate University of Chinese Academy of Sciences,Beijing 100039,China |
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| Abstract: | To solve the problem in screening the candidate target proteins of poor solubility drugs with limited immobilization function groups by traditional chemical proteomics method,a chemical proteomics method for screening candidate proteins targets,with insoluble drugs particles directly as matrix,was explored.Compared with the traditional methods,the support free protocol could not only avoid the problems caused by matrices and linkers,but also maintain all active sites of drugs without immobilization.The prot... |
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| Keywords: | dexamethasone chemical proteomics drug proteins targets insoluble drugs |
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