Development of non-secosteroidal vitamin D receptor ligands based on novel hydrophobic core structure
| Project/Area Number |
21790110
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokyo Medical and Dental University |
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Principal Investigator |
FUJII Shinya Tokyo Medical and Dental University, 大学院・疾患生命科学研究部, 助教 (60389179)
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| Project Period (FY) |
2009 – 2010
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| Project Status |
Completed (Fiscal Year 2010)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2009: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 薬学 / 有機化学 / 生理活性 / 医薬化学 / 核内受容体 / ホウ素クラスター / ノンセコステロイド / ビタミンD |
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| Research Abstract |
Activated vitamin D (1α,25(OH)_2D_3) regulates various physiological processes by binding to its specific nuclear receptor vitamin D receptor (VDR). In this research, potent non-secosteroidal VDR ligands bearing a boron cluster as hydrophobic core structure were developed. Structural development of boron cluster derivatives revealed structure-activity relationship of novel VDR ligands bearing spherical hydrophobic core.
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Report
(3 results)
Research Products
(37 results)
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[Journal Article] Crystal structure, docking study and structure-activity relationship of carborane-containing androgen receptor antagonist 3-(12-hydroxymethyl-1,12-dicarba- closo-do decaboran-1-yl)benzonitrile.
Author(s)
Kiminori Ohta, Tokuhito Goto, Shinya Fujii, Masatoshi Kawahata, Akifumi Oda, Shigeru Ohta, Kentaro Yamaguchi, Shuichi Hirono, Yasuyuki Endo
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Journal Title
Bioorg.Med.Chem. in press.
Related Report
Peer Reviewed
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[Presentation] ホウ素クラスターを疎水性骨格とする新規非セコステロイド型ビタミンD誘導体-受容体結合様式と構造展開-2010
Author(s)
藤井晋也, 増野弘幸, 垰田善之, 加納敦, 中林誠, 伊藤暢聡, 河内恵美子, 清水正人, 棚谷綾, 平野智也, 影近弘之
Organizer
日本レチノイド研究会第21回学術集会
Place of Presentation
大阪医科大学 高槻市(大阪)
Year and Date
2010-11-13
Related Report
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