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《Progress in Pharmaceutical Sciences》 2017-01
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Progress in Technologies for Affinity Probe-based Drug Targets Discovery

HE Yafeng;CHEN Hao;School of Chemistry and Chemical Engineering,State Key Laboratory of Coordination Chemistry,Nanjing University;  
Drug target identification is a very crucial step for pharmaceutical research. Affinity-based probe is one of the most commonly used approaches to identify drug targets. The method identifies drug target at molecular level and also provides direct evidence for molecular mechanism of drugs at cellular level. Based on the strategies for constructing DNA probes and small molecule drug probes, this paper discussed in details about recent progress in the identification of DNA damage recognition proteins and briefly introduced the mainstream technologies for exploring small molecule targets. As the most important part of probe-based drug discovery strategy, rational design of DNA or small molecule drug probes directly correlates with method operability and reliability of the finalresults as well. The experiences in constructing DNA and small molecule drug probes were summarized from different perspectives, ranging from traditional affinity purification approach to highly effective covalent coupling by photoaffinity reaction. These methodologies and insights will provide us with a rich pool of tools for investigating DNA damage related proteome and cellular processes of small molecule drugs, improving our understanding of drugs mechanisms at molecular level.
【Fund】: 科技部重点项目(973 No.2015CB856303);; 国家自然科学基金(No.91013009)
【CateGory Index】: R927
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