| 聚腺苷二磷酸核糖聚合酶-1抑制剂高通量筛选模型 |
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| 引用本文： | 柳军,张陆勇. 聚腺苷二磷酸核糖聚合酶-1抑制剂高通量筛选模型[J]. 中国药理学通报, 2007, 23(1): 124-127 |
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| 作者姓名： | 柳军 张陆勇 |
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| 作者单位： | 中国药科大学新药筛选中心,南京,江苏,210009 |
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| 基金项目： | 国家高技术研究发展计划(863计划);教育部跨世纪优秀人才培养计划 |
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| 摘 要： | 目的建立体外聚腺苷二磷酸核糖聚合酶-1[Poly(ADP-ribose)polymerase-1,PARP-1]抑制剂的高通量筛选模型,筛选潜在的PARP-1抑制剂。方法将PARP-1、裸DNA与底物NAD+反应,再将剩余底物NAD+转化为荧光物质,通过测定其荧光强度来决定PARP-1的活性,并以此筛选PARP-1的抑制剂。建立384孔板的高通量筛选模型,对9280个化合物(包括合成化合物、天然产物、微生物发酵提取物)组成的随机库进行体外筛选。结果筛选出148个活性化合物对PARP-1的抑制作用大于70%,最终确定3个化合物具有较高的抑制活性。结论建立的PARP-1抑制剂高通量筛选模型具有灵敏度高、快速、微量、准确的特点。
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| 关 键 词： | PARP-1 抑制剂 高通量筛选 |
| 文章编号： | 1001-1978（2007）01-0124-04 |
| 修稿时间： | 2006-07-07 |
HTS model for Poly(ADP-ribose) polymerase-1 inhibitors |
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| LIU Jun,ZHANG Lu-yong. HTS model for Poly(ADP-ribose) polymerase-1 inhibitors[J]. Chinese Pharmacological Bulletin, 2007, 23(1): 124-127 |
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| Authors: | LIU Jun ZHANG Lu-yong |
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| Affiliation: | National Drug Screening Laboratory, China Pharmaceutical University, Nanjing 210038,China |
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| Abstract: | Aim To introduce a high throughput screen model for PARP-1 inhibitors. Methods Setting up an assay for PARP-1 activity relies on the conversion of NAD~ into a highly fluorescent compound. The inhibitory effects of 9 280 samples(including pure organic compounds, extracts from plants and extracts from microorganism)were screened by the high throughout assay. Results 148 compounds had inhibitory effects over 70%. Ultimately, three inhibitors were identified as PARP-1 inhibitor with high activity.Conclusion The high throughput screening was a highly sensitive, inexpensive, and operationally simple assay method in identifying PARP-1 inhibitors. |
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| Keywords: | PARP-1 |
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