2013 Fiscal Year Final Research Report
Development of novel vitamin K derivatives and elucidation of their biological functions
| Project/Area Number |
23659051
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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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 |
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| Co-Investigator(Renkei-kenkyūsha) |
FUJII Shinya 東京医科歯科大学, 生体材料工学研究所, 助教 (60389179)
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| Project Period (FY) |
2011 – 2013
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| Keywords | ビタミンK / メナキノン / 酸化誘導体 / 癌細胞 / 増殖抑制 / 抗炎症効果 |
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| Research Abstract |
Recently, novel biological properties of vitamin K, including function as some nuclear receptor ligand and inhibitory activity of cancer cell proliferation. In this study, we examined to develop novel vitamin K derivatives in order to clarify the detailed biological functions of vitamin K and to apply them to clinical utility. Based on our hypothesis that vitamin K (menaquinones) would be metabolized to yield an active substance for some vitamin K functions, we designed the derivatives bearing an polar functional group at the terminal of the side chain. As a result, we developed the efficient synthetic method for vitamin K metabolites, K acid I and II, and synthesized systematically the oxidative derivatives of vitamin K with various length of the side chain. Some of these novel derivatives inhibited the proliferation of some cancer cells in vitro, and showed anti-inflammatory effects in vivo.
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[Journal Article] Retinoic acid receptor agonists regulate expression of ATP-binding cassette transporter G1 in macrophages2012
Author(s)
Ayaori, M.; Yakushiji, E.; Ogura, M.; Nakaya, K.; Hisada, T.; Uto-Kondo, H.; Takiguchi, S.; Terao, Y.; Sasaki, M.; Komatsu, T.; Iizuka, M.; Yogo, M.; Uehara, Y.; Kagechika, H.; Nakanishi, T.; Ikewaki, K
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Journal Title
Biochim. Biophys. Acta- Mol Cell Biol. Lipids
Volume: 1821
Pages: 561-572
DOI
Peer Reviewed
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[Journal Article] Boron Cluster-based Development of Potent Non-Secosteroidal Vitamin D Receptor Ligands : Direct Observation of Hydrophobic Interaction between Protein Surface and Carborane2011
Author(s)
Fujii, S.; Masuno, H.; Taoda, H.; Kano, A.; Wongmayura, A.; Nakabayashi, M.; Ito, N.; Shimizu, M.; Kawachi, E.; Hirano, T.; Endo, Y.; Tanatani, A.; Kagechika, H
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Journal Title
J. Am. Chem. Soc
Volume: 133
Pages: 20933-20941
DOI
Peer Reviewed
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[Presentation] Development of Various Functional Molecules Based on Hydrophobic and Fluorescent Scaffolds2012
Author(s)
Hirano, T., Fujii, S., Mori, S., Tanatani, A., Kagechika, H
Organizer
The 1st Official Conference of the International Chemical Biology Society (ICBS2012)
Place of Presentation
Boston, USA
Year and Date
20121004-05
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[Presentation] Design and Synthesis of Novel VDR Ligand having A Spherical Hydrophobic Structure2012
Author(s)
Masuno, H., Fujii, S., Wongmayura, A., Ito, S., Kawachi, E., Tanatani, A., Kagechika, H
Organizer
Vitamin D Workshop
Place of Presentation
Houston, USA
Year and Date
20120619-22
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[Presentation] Development of Novel AR Antagonists Active in LNCaP Cells with Mutated Androgen Receptor2011
Author(s)
Yamada, A., Fujii, S., Tomita, K., Nagano, M., Harayama, T., Ohta, K., Endo, Y., Kagechika, H
Organizer
AIMECS11
Place of Presentation
Tokyo
Year and Date
20111129-1202
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[Presentation] Development of novel carborane-based androgen receptor antagonists effective for mutated receptor2011
Author(s)
Yamada, A., Fujii, S., Tomita, K., Nagano, M., Harayama, T., Ohta, K., Endo, Y., Kagechika, H
Organizer
IME Boron XIV
Place of Presentation
Niagara Falls, Canada
Year and Date
20110911-15
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[Presentation] Development and structural basis of novel non-secosteroidal VDR ligands based on hydrophobic carborane cage2011
Author(s)
Fujii, S., Masuno, H., Nakabayashi, M., Hirano, T., Kawachi, E., Ito, N., Kagechika, H
Organizer
IME Boron XIV
Year and Date
20110911-15
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