developmentofahighthroughputfluorescencepolarizationassayforthediscoveryofezh2eedinteractioninhibitors
文献类型：期刊论文
| 作者 | Zhu Maorong1; Du Daohai2; Hu Junchi2; Li Lianchun2; Liu Jingqiu2; Ding Hong2 ; Kong Xiangqian2; Jiang Hualiang2; Chen Kaixian2; Luo Cheng2
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| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2018 |
| 卷号 | 39期号:2页码:302 |
| 关键词 | PRC2 EZH2 EED protein-protein interaction fluorescence polarization high-throughput screening apomorphine hydrochloride oxyphenbutazone nifedipine ergonovine maleate |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2017.59 |
| 英文摘要 | Aberrant activity of enhancer of zeste homolog 2 (EZH2) is associated with a wide range of human cancers. The interaction of EZH2 with embryonic ectoderm development (EED) is required for EZH2's catalytic activity. Inhibition of the EZH2-EED complex thus represents a novel strategy for interfering with the oncogenic potentials of EZH2 by targeting both its catalytic and non-catalytic functions. To date, there have been no reported high-throughput screening (HTS) assays for inhibitors acting at the EZH2-EED interface. In this study, we developed a fluorescence polarization (FP)-based HTS system for the discovery of EZH2-EED interaction inhibitors. The tracer peptide sequences, positions of fluorescein labeling,and a variety of physicochemical conditions were optimized. The high Z' factors (>0.9) at a variety of DMSO concentrations suggested that this system is robust and suitable for HTS. The minimal sequence requirement for the EZH2-EED interaction was determined by using this system. A pilot screening of an in-house compound library containing 1600 FDA-approved drugs identified four compounds (apomorphine hydrochloride, oxyphenbutazone, nifedipine and ergonovine maleate) as potential EZH2-EED interaction inhibitors. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/288333]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学技术大学 2.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Zhu Maorong,Du Daohai,Hu Junchi,et al. developmentofahighthroughputfluorescencepolarizationassayforthediscoveryofezh2eedinteractioninhibitors[J]. actapharmacologicasinica,2018,39(2):302. |
| APA | Zhu Maorong.,Du Daohai.,Hu Junchi.,Li Lianchun.,Liu Jingqiu.,...&Luo Cheng.(2018).developmentofahighthroughputfluorescencepolarizationassayforthediscoveryofezh2eedinteractioninhibitors.actapharmacologicasinica,39(2),302. |
| MLA | Zhu Maorong,et al."developmentofahighthroughputfluorescencepolarizationassayforthediscoveryofezh2eedinteractioninhibitors".actapharmacologicasinica 39.2(2018):302. |
入库方式： OAI收割
来源：上海药物研究所
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