| 活性小分子化合物靶点验证方法的研究进展 |
| 投稿时间：2015-09-07 修订日期：2016-01-22 点此下载全文 |
| 引用本文：陈树强,董国强,盛春泉,张万年.活性小分子化合物靶点验证方法的研究进展[J].药学实践杂志,2016,34(2):97~102 |
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| 基金项目:国家自然科学基金(81373278) |
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| 中文摘要:随着科学的发展和时代的进步,药物化学的研究不仅仅局限于先导化合物的发现及其构效关系的研究,一些小分子药物靶点的确认正逐渐成为阻碍药物化学发展的瓶颈问题。因此,活性小分子化合物靶点的鉴定与确认也成为研究过程中最为关键和艰巨的任务,通常会起到决定性作用。本文简要总结活性小分子化合物靶点验证的现行方法,阐述通过合成探针进行靶标鉴别的手段,介绍探针的设计与合成思想,并列举应用这些方法成功找到靶点的实例。 |
| 中文关键词:亲和层析 小分子药物 靶标确认 荧光探针 |
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| Advances of validation of bioactive small molecule targets |
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| Abstract:With the development of science and the progress of age, medicinal chemistry is not only limited to the lead discovery and the structure-activity relationship studies, but also finding the target of bioactive small molecule drugs has become a tough issue to be solved. The identification and validation of bioactive small molecule targets has become the most critical and difficult task, which plays a decisive role in academic and pharmaceutical research. Herein we summarize the current methods for target identification of small molecules,and mainly discuss about the target identification method by the chemical probes. Recent cases of successful application were also introduced to demonstrate the strategy of probe synthesis and design. |
| keywords:pulldown small molecule drugs target identification fluorescent probes |
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