Development of estrogen receptor degrader and analysis of drug-induced cell death mechanism for breast cancer therapy
Project/Area Number |
25430164
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Tumor therapeutics
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Research Institution | The University of Tokushima (2014-2015) National Institute of Health Sciences (2013) |
Principal Investigator |
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Co-Investigator(Renkei-kenkyūsha) |
DEMIZU Yosuke 国立医薬品食品研究所, 有機化学部, 室長 (90389180)
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Project Period (FY) |
2013-04-01 – 2016-03-31
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Project Status |
Completed (Fiscal Year 2015)
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Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2013: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
|
Keywords | 乳癌 / エストロゲン受容体 / エストロゲンレセプター |
Outline of Final Research Achievements |
Recently, we have developed a hybrid small molecule named SNIPER(ER) (Specific and Non-genetic IAP-dependent Protein Eraser for Estrogen Receptor) that induces degradation of estrogen receptor alpha (ERa) proteins via ubiquitin-proteasome system. In this study, we revealed that SNIPER(ER) induces ROS production after the ERa degradation and caused necrotic cell death of MCF-7 cells, implying a therapeutic potential of SNIPER(ER) as a lead for the treatment of ERa-positive breast cancers.
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Report
(4 results)
Research Products
(20 results)
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[Journal Article] Development of cell-penetrating R7 fragment-conjugated helical peptides as inhibitors of estrogen receptor-mediated transcription.2014
Author(s)
2.Nagakubo, T., Demizu, Y., Kanda, Y., Misawa, T., Shoda, T., Okuhira, K., Sekino., Y., Naito, M. and Kurihara, M
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Journal Title
Bioconjug Chem.
Volume: 25
Issue: 11
Pages: 1921-24
DOI
Related Report
Peer Reviewed
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[Journal Article] Cancer cell death induced by novel small molecules degrading the TACC3 protein via the ubiquitin proteasome pathway.2014
Author(s)
1.Ohoka, N., Nagai, K., Hattori, T., Okuhira, K., Shibata, N., Cho, N. and Naito, M
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Journal Title
Cell Death Dis.
Volume: 5
Issue: 11
Pages: e1513-e1513
DOI
Related Report
Peer Reviewed / Open Access / Acknowledgement Compliant
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[Journal Article] Design and synthesis of tamoxifen derivatives as a selective estrogen receptor down-regulator.2014
Author(s)
Shoda, T., Okuhira, K., Kato, M., Demizu, Y., Inoue, H., Naito, M., and Kurihara, M.
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Journal Title
Bioorg Med Chem Lett
Volume: 24
Issue: 1
Pages: 87-89
DOI
Related Report
Peer Reviewed
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[Journal Article] Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells.2013
Author(s)
Okuhira, K., Demizu, Y., Hattori, T., Ohoka, N., Shibata, N., Nishimaki-Mogami, T., Okuda, H., Kurihara, M., Natiro, M.
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Journal Title
Cancer Science
Volume: 104
Issue: 11
Pages: 1492-1498
DOI
Related Report
Peer Reviewed
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[Presentation] 網羅的人工ユビキチン修飾システムの構築2016
Author(s)
大岡 伸通, 伊東 昌宏, 奥平 桂一郎, 永井 克典, 柴田 識人, 服部 隆行, 長 展生, 内藤 幹彦
Organizer
日本薬学会第136年会
Place of Presentation
パシフィコ横浜(神奈川県横浜市)
Year and Date
2016-03-26
Related Report
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[Presentation] エストロゲン受容体転写活性化阻害ペプチドの創製2015
Author(s)
出水 庸介, 長久保 貴哉, 三澤 隆史, 諫田 泰成, 奥平 桂一郎, 関野 祐子, 内藤 幹彦, 栗原 正明
Organizer
日本薬学会第135年会
Place of Presentation
神戸学院大学(兵庫県・神戸市)
Year and Date
2015-03-25 – 2015-03-28
Related Report
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