| Project/Area Number |
21590022
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | Teikyo University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
TAKANO Masashi 帝京大学, 薬学部, 助教 (50386611)
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| Co-Investigator(Renkei-kenkyūsha) |
SAWADA Daisuke 帝京大学, 薬学部, 准教授 (00338691)
SUGIYAMA Toru 東京大学, 総合文化研究科, 助教 (40242036)
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| Project Period (FY) |
2009 – 2011
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| Project Status |
Completed (Fiscal Year 2011)
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| Budget Amount *help |
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2011: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2010: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2009: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | 有機化学 / 薬学 / 合成化学 / 生理活性 / 活性型ビタミンD3 / ビタミンD受容体 / タキステロール / 活性型ビタミンD_3 / ビタミンD受容体(VDR) / 19-ノルタキステロール / 14-エピ-活性型ビタミンD_3 / 19-ノルプレビタミンD_3 |
|---|
| Research Abstract |
As a novel skeleton of vitamin D working on bone formation, 14-epi-2α-methyl-1α, 25-dihydroxy-19-norprevitamin D_3 has been synthesized. Interestingly, we found that the new compound epimerizes to 14-epi-2α-methyl-1α, 25-dihydroxy-19-nortachysterol by acidic catalysts, and the tachysterol analog showed potent osteocalcin promoter transactivation activity through the vitamin D receptor. Next, we developed a direct synthetic route to the epimerized compound to obtain enough amount of the tachysterol analog for in vivo studies. X-ray co-crystallographic studies explained an unprecedented binding mode of the tachysterol to the vitamin D receptor.
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