Development of molecular probes for steroid hormone receptor functions
| Project/Area Number |
24590137
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Ochanomizu University |
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Principal Investigator |
TANATANI Aya お茶の水女子大学, 大学院人間文化創成科学研究科, 准教授 (40361654)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | ステロイドホルモン / 核内受容体 / アンドロゲン / プロゲステロン / アンタゴニスト / 蛍光性リガンド / クマリン / 光学分割 / 蛍光プローブ / フタラジノン |
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| Outline of Final Research Achievements |
In this study, the specific ligands and fluorescence probes for steroid hormone nuclear receptors were developed.
(1) Phthalazinone derivatives were developed as novel androgen antagonists, and acted as antagonists towards both wild-type and mutated ARs. As progesterone antagonists, compounds bearing a carborane or adamantane as the hydrophobic pharmacophore were developed.
(2) Coumarine derivatives were developed as fluorescent progesterone antagonists, whose fluorescence intensity was strongly increased by binding to progesterone receptor. Coumarine derivatives with androgen antagonistic activity were also developed.
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Report
(4 results)
Research Products
(46 results)
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[Journal Article] Redox-Responsive Conformational Alteration of Aromatic Amides Bearing N-Quinonyl System2012
Author(s)
Iwao Okamoto, Yusuke Takahashi, Mika Sawamura, Mio Matsumura, Hyuma Masu, Kosuke Katagiri, Isao Azumaya, Masanori Nishino, Yukari Kohama, Nobuyoshi Morita, Osamu Tamura, Hiroyuki Kagechika, Aya Tanatani
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Journal Title
Tetrahedron
Volume: 68
Issue: 27-28
Pages: 5346-5355
DOI
Related Report
Peer Reviewed
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[Presentation] Formation of Chiral Helical Chain Structures of N,N’-bis(ortho-substituted phenyl)squaramides in the Crystals2013
Author(s)
Midori Kanda, Shinya Fujii, Mio Matsumura, Kosuke Katagiri, Hyuma Masu, Isao Azumaya, Hiroyuki Kagechika, Aya Tanatani
Organizer
ISMSC-8
Place of Presentation
Arlinton, VA, USA
Related Report
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