Orthogonal assays for the identification of inhibitors of the single-stranded nucleic acid binding protein YB-1
文献类型：期刊论文
| 作者 | Trevarton, Alexander J.1; Zhou, Yan2,3; Yang, Dehua2,3 ; Rewcastle, Gordon W.4,5; Flanagan, Jack U.4,5; Braithwaite, Antony6,7; Shepherd, Peter R.1,5; Print, Cristin G.1,5; Wang, Ming-Wei2,3,8; Lasham, Annette1,5
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| 刊名 | ACTA PHARMACEUTICA SINICA B
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| 出版日期 | 2019-09-01 |
| 卷号 | 9期号:5页码:997-1007 |
| 关键词 | Cancer YB-1 Luciferase AlphaScreen Transcription factor Single-stranded DNA |
| ISSN号 | 2211-3835 |
| DOI | 10.1016/j.apsb.2018.12.011 |
| 通讯作者 | Print, Cristin G.(c.print@auckland.ac.nz) ; Wang, Ming-Wei(mwwang@simm.ac.cn) ; Lasham, Annette(a.lasham@auckland.ac.nz) |
| 英文摘要 | We have previously shown that high expression of the nucleic acid binding factor YB-1 is strongly associated with poor prognosis in a variety of cancer types. The 3-dimensional protein structure of YB-1 has yet to be determined and its role in transcriptional regulation remains elusive. Drug targeting of transcription factors is often thought to be difficult and there are very few published high-throughput screening approaches. YB-1 predominantly binds to single-stranded nucleic acids, adding further difficulty to drug discovery. Therefore, we have developed two novel screening assays to detect compounds that interfere with the transcriptional activation properties of YB-1, both of which may be generalizable to screen for inhibitors of other nucleic acid binding molecules. The first approach is a cell-based luciferase reporter gene assay that measures the level of activation of a fragment of the E2F1 promoter by YB-1. The second approach is a novel application of the AlphaScreen system, to detect interference of YB-1 interaction with a single-stranded DNA binding site. These complementary assays examine YB-1 binding to two discrete nucleic acid sequences using two different luminescent signal outputs and were employed sequentially to screen 7360 small molecule compounds leading to the identification of three putative YB-1 inhibitors. (C) 2019 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. |
| WOS关键词 | COLD-SHOCK DOMAIN ; DRUG-RESISTANCE ; MESSENGER-RNA ; EXPRESSION ; PROLIFERATION ; ONCOPROTEIN ; APOPTOSIS ; PATHWAY |
| 资助项目 | Health Research Council of New Zealand (China)[IRF213] ; Health Research Council of New Zealand (China)[13-1019] ; Ministry of Science and Technology of China[2014DFG32200] ; Shanghai Science and Technology Development Fund (China)[15DZ2291600] ; Thousand Talents Program in China[[2011]166] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000487282700010 |
| 出版者 | INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/288572]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Print, Cristin G.; Wang, Ming-Wei; Lasham, Annette |
| 作者单位 | 1.Univ Auckland, Dept Mol Med & Pathol, Auckland, New Zealand 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 4.Auckland Canc Soc, Res Ctr, Auckland, New Zealand 5.Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland, New Zealand 6.Univ Otago, Dunedin Sch Med, Dept Pathol, Dunedin, New Zealand 7.Univ Otago, Maurice Wilkins Ctr Mol Biodiscovery, Dunedin, New Zealand 8.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Trevarton, Alexander J.,Zhou, Yan,Yang, Dehua,et al. Orthogonal assays for the identification of inhibitors of the single-stranded nucleic acid binding protein YB-1[J]. ACTA PHARMACEUTICA SINICA B,2019,9(5):997-1007. |
| APA | Trevarton, Alexander J..,Zhou, Yan.,Yang, Dehua.,Rewcastle, Gordon W..,Flanagan, Jack U..,...&Lasham, Annette.(2019).Orthogonal assays for the identification of inhibitors of the single-stranded nucleic acid binding protein YB-1.ACTA PHARMACEUTICA SINICA B,9(5),997-1007. |
| MLA | Trevarton, Alexander J.,et al."Orthogonal assays for the identification of inhibitors of the single-stranded nucleic acid binding protein YB-1".ACTA PHARMACEUTICA SINICA B 9.5(2019):997-1007. |
入库方式： OAI收割
来源：上海药物研究所
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