手性药物合成中酶的高通量筛选进展  

High-throughput screening progress of the enantioselective enzymes in the preparation of chiral drugs

作　　者：宋明[1] 张新[1] 游松[1] 

机构地区：[1]沈阳药科大学生命科学与生物制药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2013年第4期318-328,共11页Journal of Shenyang Pharmaceutical University

基　　金：辽宁省教育厅资助项目(L2010525);国家创新药物重大专项(2009ZX09301-012);沈阳市手性药物生物催化合成重点实验室项目(F11-243-1-00)

摘　　要：目的介绍手性药物合成中酶的高通量筛选方法的进展。方法根据近年发表的关于手性药物合成中酶的高通量筛选文献共30篇,对其进行综述。结果介绍了一系列的立体选择性酶筛选方法。包括化学发光和荧光法,pH指示剂法,酶偶联分析法等,这些方法都体现了高通量的原则,即快速、高效、可靠。结论高通量筛选方法对于寻找新的酶和生物催化剂意义重大。Objective To review the current progress on high-throughput screening （HTS） to identify enanti- oselective enzymes for chiral drugs. Methods Review was given based on relative references about HTS. Re- sults In this review, a series of HTS approaches for enantioselective enzymes were covered, including UV/ Vis spectroscopy-and fluorescence-based assays, pH-indicators screening and enzyme-coupled ee screening systems as well as other methods. The approaches were proved to be fast, efficient and reliable for the identi- fication of desired enzyme variants within large mutant libraries. Conclusions HTS approaches have recently emerged as a powerful tool for screening enantioselective enzyme libraries due to their high speed and sensi- tivity.

关 键 词：高通量筛选 立体选择性 生物催化 

分 类 号：R914[医药卫生—药物化学]