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Study and development of a 14-epi-tachysterol skeleton and enhancing bone formation via flexibility of ligand binding domain of vitamin D receptor

Research Project

Project/Area Number 24590021
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Chemical pharmacy
Research InstitutionTeikyo University

Principal Investigator

KITTAKA Atsushi  帝京大学, 薬学部, 教授 (00214833)

Co-Investigator(Kenkyū-buntansha) TAKANO Masashi  帝京大学, 薬学部, 助教 (50386611)
Co-Investigator(Renkei-kenkyūsha) SAWADA Daisuke  帝京大学, 薬学部, 准教授 (00338691)
SUGIYAMA Toru  東京大学, 大学院総合文化研究科, 助教 (40242036)
SAKAKI Toshiyuki  富山県立大学, 工学部, 教授 (70293909)
Project Period (FY) 2012-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywords薬学 / 有機化学 / 合成化学 / ビタミンD / 骨粗鬆症治療薬 / タキステロール / 生物活性 / ビタミンD受容体 / 生体分子 / 生理活性
Outline of Final Research Achievements

Vitamin D biosynthesis undergoes in human skin with sunshine, and tachysterol is produced as one of the byproducts during the process. Tachysterol is a chemically unstable compound, and it is difficult to study its property. In this project, we synthesized stable tachysterol analogs and clarified their binding mode for human vitamin D receptor (hVDR) by X-ray analysis, and we planned to create desirable osteoporosis chemotherapy. We found that the 19-methyl group is unnecessary for better binding with hVDR, and functionalization of active vitamin D3, which strengthen biological activity, was not suitable for the tachysterol analogs. Although stable tachysterol analogs with a diene system were also synthesized, we found it was not effective on biological activity.

Report

(4 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Research-status Report
  • 2012 Research-status Report
  • Research Products

    (97 results)

All 2015 2014 2013 2012 Other

All Journal Article (34 results) (of which Peer Reviewed: 26 results,  Acknowledgement Compliant: 5 results,  Open Access: 3 results) Presentation (55 results) (of which Invited: 7 results) Book (2 results) Remarks (6 results)

  • [Journal Article] 19-Norvitamin D Analogs for Breast Cancer Therapy2015

    • Author(s)
      Yotaro Matsumoto, Atsushi Kittaka, and Tai C. Chen
    • Journal Title

      Canadian Journal of Physiol. Pharmacol.

      Volume: 93 Issue: 6 Pages: 123-149

    • DOI

      10.1139/cjpp-2014-0356

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Modified Deazaguanines for the Synthesis of PNA2015

    • Author(s)
      Toru Sugiyama, Keiko Kuwata, Yasutada Imamura, Yosuke Demizu, Masaaki Kurihara, Masashi Takano, and Atsushi Kittaka
    • Journal Title

      Peptide Science 2014

      Volume: 51 Pages: 87-88

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] A Peptide Nucleic Acid to Reduce Type I Collagen Production by Fibroblast Cells2015

    • Author(s)
      Yasutada Imamura, Suzuka Tsuboi, Toru Sugiyama, Atsushi Kittaka, and Yonchol Shin
    • Journal Title

      Open Journal of Medicinal Chemistry 2015

      Volume: 5 Issue: 01 Pages: 1-8

    • DOI

      10.4236/ojmc.2015.51001

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Synthesis and metabolic studies of 1α,2α,25-, 1α,4α,25- and 1α,4β,25-trihydroxyvitamin D32015

    • Author(s)
      Masashi Takano, Daisuke Sawada, Kaori Yasuda, Miyu Nishikawa, Akiko Takeuchi, Ken-ichiro Takagi, Kyohei Horie, G. Satyanarayana Reddy, Tai C. Chen, Toshiyuki Sakaki, and Atsushi Kittaka
    • Journal Title

      J. Steroid Biochem. Mol. Biol.

      Volume: 148 Pages: 34-37

    • DOI

      10.1016/j.jsbmb.2014.09.021

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Synthesis and Preliminary Biological Evaluation of 2-[3-(Tetrazolyl)propyl]-1α,25-dihydroxy-19-norvitamin D32015

    • Author(s)
      Masashi Takano, Erika Higuchi, Kazunari Higashi, Keisuke Hirano, Akiko Takeuchi, Daisuke Sawada, and Atsushi Kittaka
    • Journal Title

      Heterocycles

      Volume: 90 Issue: 2 Pages: 1274-1287

    • DOI

      10.3987/com-14-s(k)108

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] ビタミンD受容体リガンドの創製2015

    • Author(s)
      橘高敦史、澤田大介
    • Journal Title

      ファルマシア

      Volume: 51 Pages: 196-200

    • NAID

      130007448010

    • Related Report
      2014 Annual Research Report
  • [Journal Article] 細胞選択的及び遺伝子選択的活性を有するビタミンD誘導体の生物活性評価2015

    • Author(s)
      石澤通康、高野真史、橘高敦史、坂根里枝、須原義智、山田幸子、槇島 誠
    • Journal Title

      ビタミン

      Volume: 89 Pages: 39-39

    • Related Report
      2014 Annual Research Report
  • [Journal Article] Vitamin D against Cancer2014

    • Author(s)
      Tai C. Chen, Atsushi Kittaka, and Gunnar Norstedt
    • Journal Title

      International Innovation

      Volume: 157 Pages: 18-19

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] The Vitamin D analog, MART-10, represses metastasis potential via downregulation of epithelial-mesenchymal transition in pancreatic cancer cells2014

    • Author(s)
      Kun-Chun Chiang, Chun-Nan Yeh, Jun-Te Hsu, Yi-Yin Jan, Li-Wei Chen, Sheng-Fong Kuo, Masashi Takano, Atsushi Kittaka, Tai-C Chen, Wen-Tsung Chen, Jong-Hwei S.Pang, Ta-Sen Yeh, and Horng-Heng Juang
    • Journal Title

      Cancer Letters

      Volume: 354 Issue: 2 Pages: 235-244

    • DOI

      10.1016/j.canlet.2014.08.019

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis and properties of 14-epi-1α,25-dihydroxy-19-nortachysterol and its 2-substituted derivatives2014

    • Author(s)
      Daisuke Sawada and Atsushi Kittaka
    • Journal Title

      Current Topics in Medicinal Chemistry

      Volume: 14 Issue: 21 Pages: 2454-2459

    • DOI

      10.2174/1568026615666141208103741

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Chemopreventive and Chemotherapeutic Effect of Dietary Supplementation of Vitamin D on Cholangiocarcinoma in a Chemical-Induced Animal Model2014

    • Author(s)
      Kun-Chun Chiang, Chun-Nan Yeh, Kun-Ju Lin, Li-Jen Su, Tzu-Chen Yen, Jong-Hwei S. Pang, Atsushi Kittaka, Chi-Chin Sun, Miin-Fu Chen, Yi-Yin Jan, Horng-Heng Juang, Ta-Sen Yeh, and Tai C. Chen
    • Journal Title

      Oncotarget

      Volume: 5 Pages: 3849-3861

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Sequence-Specific Cleavage of DNA by β-Peptide Nucleic Acid Bearing a Pendant Metal Complex2014

    • Author(s)
      Toru Sugiyama, Keiko Kuwata, Yasutada Imamura, Yosuke Demizu, Masaaki Kurihara, Masashi Takano, and Atsushi Kittaka
    • Journal Title

      Peptide Science 2013

      Volume: 50 Pages: 369-370

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] 2α位にテトラゾールプロピル基を有する19-ノル型ビタミンD3の合成と生物活性評価2014

    • Author(s)
      高野真史、樋口恵理香、竹内明子、澤田大介、橘高敦史
    • Journal Title

      ビタミン

      Volume: 88 Pages: 244-244

    • Related Report
      2014 Annual Research Report
  • [Journal Article] メチルステロール酸化酵素SC4MOLによる2位置換基付加型ビタミンD誘導体の代謝2014

    • Author(s)
      安田佳織、岩永由麻、小川和亮、生城真一、鎌倉昌樹、高野真史、齋藤 望、橘高敦史、藤島利江、太田美穂、榊 利之
    • Journal Title

      ビタミン

      Volume: 88 Pages: 243-243

    • Related Report
      2014 Annual Research Report
  • [Journal Article] CYP24A1 as a Potential Target for Cancer Therapy2014

    • Author(s)
      Toshiyuki Sakaki, Kaori Yasuda, Atsushi Kittaka, Keiko Yamamoto, and Tai C. Chen
    • Journal Title

      Anti-Cancer Agents Med. Chem.

      Volume: 14 Issue: 1 Pages: 97-108

    • DOI

      10.2174/18715206113139990307

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Design and synthesis of 2α-(tetrazolylethyl)-1α,25-dihydroxyvitamin D3 as a high affinity ligand for vitamin D receptor2014

    • Author(s)
      Miki Matsuo, Asami Hasegawa, Masashi Takano, Hiroshi Saito, Shinji Kakuda, Kenichiro Takagi, Eiji Ochiai, Kyohei Horie, Midori Takimoto-Kamimura, Kazuya Takenouchi, Daisuke Sawada, and Atsushi Kittaka
    • Journal Title

      J. Steroid Biochem. Mol. Biol.

      Volume: in press Pages: 201-203

    • DOI

      10.1016/j.jsbmb.2013.09.001

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] MART-10, a Less Calcemic Vitamin D Analog, Is More Potent Than 1,25-Dihydroxyvitamin D3 in Inhibiting the Metastatic Potential of MCF-7 Breast Cancer Cells in Vitro2014

    • Author(s)
      Kun-Chun Chiang, Shin-Cheh Chen, Chun-Nan Yeh, Jong-Hwei S. Pang, Shih-Che Shen, Jun-Te Hsu, Yu-Yin Liu, Li-Wei Chen, Sheng-Fong Kuo, Masashi Takano, Atsushi Kittaka, Chi-Chin Sun, Horng-Heng Juang, and Tai C. Chen
    • Journal Title

      J. Steroid Biochem. Mol. Biol.

      Volume: 139 Pages: 54-60

    • DOI

      10.1016/j.jsbmb.2013.10.005

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis and Biological Activity of 1α,2α,25-Trihydroxyvitamin D<sub>3</sub>: Active Metabolite of 2α-(3-Hydroxypropoxy)-1α,25-dihydroxyvitamin D<sub>3</sub> by Human CYP3A42014

    • Author(s)
      Masashi Takano, Saori Ohya, Kaori Yasuda, Miyu Nishikawa, Akiko Takeuchi, Daisuke Sawada, Toshiyuki Sakaki, and Atsushi Kittaka
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 62 Issue: 2 Pages: 182-184

    • DOI

      10.1248/cpb.c13-00646

    • NAID

      130003390755

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis of 2α-Heteroarylalkyl Active Vitamin D3 with Therapeutic Effect on Enhancing Bone Mineral Density in vivo2013

    • Author(s)
      Miki Matsuo, Asami Hasegawa, Masashi Takano, Hiroshi Saito, Shinji Kakuda, Takayuki Chida, Ken-ichiro Takagi, Eiji Ochiai, Kyohei Horie, Yoshifumi Harada, Midori Takimoto-Kamimura, Kazuya Takenouchi, Daisuke Sawada, and Atsushi Kittaka
    • Journal Title

      ACS Med. Chem. Lett.

      Volume: 4 Issue: 7 Pages: 671-674

    • DOI

      10.1021/ml400098w

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis of β-Chiral Peptide Nucleic Acids Bearing Lysine Side Chains2013

    • Author(s)
      Toru Sugiyama, Yasutada Imamura, Yosuke Demizu, Masaaki Kurihara, Masashi Takano, and Atsushi Kittaka
    • Journal Title

      Peptide Science 2012

      Volume: 49 Pages: 385-386

    • NAID

      10031161665

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] MART-10, a Novel Vitamin D Analog, Inhibits Head and Neck Squamous Carcinoma Cells Growth through Cell Cycle Arrest at G0/G1 with Upregulation of p21 and p27 and Downregulation of Telomerase2013

    • Author(s)
      Kunchun Chiang, Chun-Nan Yeh, Jun-Te Hsu, Li-Wei Chen, Sheng-Fong Kuo, Chi-Chin Sun, Cheng-Cheng Huang, Jong-Hwei S. Pang, John N. Flanagan, Masashi Takano, Atsushi Kittaka, Horng-Heng Juang, Shih-Wei Yang and Tai C. Chen
    • Journal Title

      J. Steroid Biochem. Mol. Biol.

      Volume: 138 Pages: 427-434

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] 14-エピ-タキステロール類の合成とVDR結合様式の解明2013

    • Author(s)
      澤田大介、堀江恭平、落合鋭士、竹内明子、角田真二、上村みどり、橘高敦史
    • Journal Title

      ビタミン

      Volume: 87 Pages: 220-220

    • Related Report
      2013 Research-status Report
  • [Journal Article] 2α-アゾールエチル基を有する1α,25-ジヒドロキシビタミンD3の合成と生物活性評価2013

    • Author(s)
      橘高敦史、松尾実紀、長谷川麻美、高野真史、澤田大介、齋藤 博、角田真二、高木健一郎、落合鋭士、堀江恭平、上村みどり、竹之内一弥
    • Journal Title

      ビタミン

      Volume: 87 Pages: 652-652

    • Related Report
      2013 Research-status Report
  • [Journal Article] Chiral peptide nucleic acids with a substituent in the N-(2-Aminoethy) glycine backbone2013

    • Author(s)
      Toru Sugiyama and Atsushi Kittaka
    • Journal Title

      Molecules

      Volume: 18 Issue: 1 Pages: 287

    • DOI

      10.3390/molecules18010287

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis of 14-epi-2α-hydroxypropoxy-1α,25-dihydroxy-19-nortachysterol and its hVDR binding2013

    • Author(s)
      Daisuke Sawada et al.
    • Journal Title

      J. Steroid Biochem. Mol. Biol.

      Volume: 133 Pages: 27-29

    • DOI

      10.1016/j.jsbmb.2012.11.014

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis of Novel C-2 Substituted Vitamin D Derivatives Having Ringed Side Chains and Their Biological Evaluation on Bone2013

    • Author(s)
      Hiroshi Saito et al.
    • Journal Title

      J. Steroid Biochem. Mol. Biol.

      Volume: 133 Pages: 3-8

    • DOI

      10.1016/j.jsbmb.2013.02.004

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Evaluation of the Potential Therapeutic Role of a New Generation of Vitamin D Analog, MART-10, in Human Pancreatic Cancer Cells in Vitro and in Vivo2013

    • Author(s)
      Kun-Chun Chiang et al.
    • Journal Title

      Cell Cycle

      Volume: 12 Issue: 8 Pages: 1316-1325

    • DOI

      10.4161/cc.24445

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis of β-Chiral Peptide Nucleic Acids and Their DNA Binding Properties2012

    • Author(s)
      Toru Sugiyama et al.
    • Journal Title

      Peptide Science 2011

      Volume: 48 Pages: 353-354

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] ヒト由来CYP24A1抵抗性ビタミンD誘導体合成とATRA耐性APL細胞分化誘導2012

    • Author(s)
      高野真史ら
    • Journal Title

      ビタミン

      Volume: 86 Pages: 243-243

    • Related Report
      2012 Research-status Report
  • [Journal Article] Synthesis and Biological Activities of 1&#945;,4&#945;,25- and 1&#945;,4&#946;,25-Trihydroxyvitamin D<sub>3</sub> and Their Metabolism by Human CYP24A1 and UDP-Glucuronosyltransferase2012

    • Author(s)
      Daisuke Sawada, Yuya Tsukuda, Kaori Yasuda, Toshiyuki Sakaki, Hiroshi Saito, Ken-ichiro Takagi, Kazuya Takenouchi, Tai C. Chen, G. Satyanarayana Reddy, and Atsushi Kittaka
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 60 Issue: 10 Pages: 1343-1346

    • DOI

      10.1248/cpb.c12-00526

    • NAID

      130001852369

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Potent 19-Norvitamin D Analogs for Prostate and Liver Cancer Therapy2012

    • Author(s)
      Atsushi Kittaka, Akihiro Yoshida, Kun-Chun Chiang, Masashi Takano, Daisuke Sawada, Toshiyuki Sakaki, and Tai C. Chen
    • Journal Title

      Future Med. Chem

      Volume: 4 (16) Issue: 16 Pages: 2049-2065

    • DOI

      10.4155/fmc.12.130

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] MART-10, a New Generation of Vitamin D Analog, Is More Potent than 1α,25-Dihydroxyvitamin D3 in Inhibiting Cell Proliferation and Inducing Apoptosis in ER+ MCF-7 Breast Cancer Cells2012

    • Author(s)
      Kun-Chun Chiang et al.
    • Journal Title

      Evidence-Based Complementary and Alternative Medicine 2012

      Volume: 2012 Pages: 1-10

    • DOI

      10.1155/2012/310872

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] 2alpha-(3-ヒドロキシプロピル)-1α,25-ジヒドロキシ-19-ノルビタミンD3(MART-10)とその類縁体の合成と制がん活性等2012

    • Author(s)
      高野真史ら
    • Journal Title

      ビタミン

      Volume: 86 Pages: 694-696

    • Related Report
      2012 Research-status Report
  • [Journal Article] Human cytochrome P450-dependent differential metabolism among three 2α-substituted-1α,25-dihydroxyvitamin D(3) analogs2012

    • Author(s)
      Yasuda, K, Ikushiro, S, Sakaki, T
    • Journal Title

      J. Steroid Biochem. Mol. Biol

      Volume: 133 Pages: 84-92

    • DOI

      10.1016/j.jsbmb.2012.09.006

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Presentation] 2α位にトリアゾリルプロピル基を有する19-ノル型ビタミンD3の合成と生物活性評価2015

    • Author(s)
      高野真史,樋口恵理香,安田佳織,榊 利之,橘高敦史
    • Organizer
      日本ビタミン学会第67回大会
    • Place of Presentation
      奈良
    • Year and Date
      2015-06-05 – 2015-06-06
    • Related Report
      2014 Annual Research Report
  • [Presentation] 強い骨密度上昇作用を有するビタミンD誘導体の代謝様式の解明2015

    • Author(s)
      遠山枝李、安田佳織、生城真一、鎌倉昌樹、高野真史、橘高敦史、榊 利之
    • Organizer
      日本ビタミン学会第67回大会
    • Place of Presentation
      奈良
    • Year and Date
      2015-06-05 – 2015-06-06
    • Related Report
      2014 Annual Research Report
  • [Presentation] 分割型ルシフェラーゼを用いたビタミンDバイオセンサーの開発2015

    • Author(s)
      真野寛生、西川美宇、安田佳織、鎌倉昌樹、生城真一、 高野真史、斉藤 望、橘高敦史、榊 利之
    • Organizer
      日本ビタミン学会第67回大会
    • Place of Presentation
      奈良
    • Year and Date
      2015-06-05 – 2015-06-06
    • Related Report
      2014 Annual Research Report
  • [Presentation] SYNTHESIS, METABOLISM, AND BIOLOGICAL ACTIVITY OF 2-[3-(TETRAZOLYL)PROPYL]- 1α,25-DIHYDROXY-19-NORVITAMIN D32015

    • Author(s)
      M. Takano, E. Higuchi, K. Yasuda, E. Tohyama, A. Takeuchi, T. Sakaki, and A. Kittaka
    • Organizer
      18th Vitamin D Workshop
    • Place of Presentation
      デルフト市、オランダ
    • Year and Date
      2015-04-21 – 2015-04-24
    • Related Report
      2014 Annual Research Report
  • [Presentation] 2-(3-トリアゾリルプロピル)-1α,25(OH)2-19-ノルビタミンD3の合成2015

    • Author(s)
      高野真史,谷川有梨紗,小川圭瞳,宮田英美,上坂博翔,阪本祥一,橘高敦史
    • Organizer
      日本薬学会 第135年会
    • Place of Presentation
      神戸
    • Year and Date
      2015-03-25 – 2015-03-28
    • Related Report
      2014 Annual Research Report
  • [Presentation] 2位にテトラゾリルプロピル基を有する19-ノル活性型ビタミンD3の合成と代謝2015

    • Author(s)
      樋口恵理香,安田佳織,高野真史,榊 利之,橘高敦史
    • Organizer
      日本薬学会 第135年会
    • Place of Presentation
      神戸
    • Year and Date
      2015-03-25 – 2015-03-28
    • Related Report
      2014 Annual Research Report
  • [Presentation] デアザグアニン誘導体を持つPNA モノマーの合成2015

    • Author(s)
      杉山 亨、桑田啓子、今村保忠、出水庸介、栗原正明、高野真史、橘高敦史
    • Organizer
      日本薬学会 第135年会
    • Place of Presentation
      神戸
    • Year and Date
      2015-03-25 – 2015-03-28
    • Related Report
      2014 Annual Research Report
  • [Presentation] 2α-(3-ヒドロキシプロピル)活性型ビタミンD3(MART-10)の合成と制がん活性2014

    • Author(s)
      高野真史,Kun-Chun Chiang,安田佳織,榊 利之,Tai C. Chen,橘高敦史
    • Organizer
      第32回メディシナルケミストリーシンポジウム
    • Place of Presentation
      神戸国際会議場
    • Year and Date
      2014-11-26 – 2014-11-28
    • Related Report
      2014 Annual Research Report
  • [Presentation] 8,9-ジヒドロ-19-ノルタキステロール誘導体の合成と生物活性評価2014

    • Author(s)
      松本洋太郎、澤田大介、竹内明子、橘高敦史
    • Organizer
      第40回反応と合成の進歩シンポジウム
    • Place of Presentation
      東北大・萩ホール
    • Year and Date
      2014-11-10 – 2014-11-11
    • Related Report
      2014 Annual Research Report
  • [Presentation] Modified Deazaguanines for the Synthesis of PNA2014

    • Author(s)
      Toru Sugiyama, Keiko Kuwata, Yasutada Imamura, Yosuke Demizu, Masaaki Kurihara, Masashi Takano, and Atsushi Kittaka
    • Organizer
      第51回ペプチド討論会
    • Place of Presentation
      徳島大学
    • Year and Date
      2014-10-22 – 2014-10-24
    • Related Report
      2014 Annual Research Report
  • [Presentation] ビタミンD: 驚異のセコステロイド骨格2014

    • Author(s)
      橘高敦史
    • Organizer
      芝浦工業大学大学院講義
    • Place of Presentation
      芝浦工業大学
    • Year and Date
      2014-10-07
    • Related Report
      2014 Annual Research Report
    • Invited
  • [Presentation] 2位置換基上にトリアゾール環を有する19-ノルビタミンD3の合成研究2014

    • Author(s)
      小川圭瞳、谷川有梨紗、宮田英美、高野真史、松本洋太郎、橘高敦史
    • Organizer
      第58回日本薬学会関東支部大会
    • Place of Presentation
      昭和薬科大学
    • Year and Date
      2014-10-04
    • Related Report
      2014 Annual Research Report
  • [Presentation] 8,9-ジヒドロ-19-ノルタキステロールの合成研究2014

    • Author(s)
      松本洋太郎、山田 徹、森 幸樹、澤田大介、橘高敦史
    • Organizer
      第58回日本薬学会関東支部大会
    • Place of Presentation
      昭和薬科大学
    • Year and Date
      2014-10-04
    • Related Report
      2014 Annual Research Report
  • [Presentation] 細胞選択的、遺伝子選択的活性を有するビタミンD誘導体の生物活性評価2014

    • Author(s)
      石澤通康、髙野真史、橘髙敦史、坂根里枝、須原義智、山田幸子、槇島 誠
    • Organizer
      第344回脂溶性ビタミン総合研究委員会
    • Place of Presentation
      東京農業大学
    • Year and Date
      2014-09-26
    • Related Report
      2014 Annual Research Report
  • [Presentation] 2α-ヘテロアリールプロピル-19-ノルビタミンD3の合成と生物活性評価2014

    • Author(s)
      高野真史、樋口恵理香、廣瀬七帆、竹内明子、澤田大介、橘高敦史
    • Organizer
      第44回複素環化学討論会
    • Place of Presentation
      札幌市民ホール
    • Year and Date
      2014-09-10 – 2014-09-12
    • Related Report
      2014 Annual Research Report
  • [Presentation] ビタミンDと太陽光2014

    • Author(s)
      橘高敦史
    • Organizer
      近畿化粧品原料協会学術講演会
    • Place of Presentation
      薬業年金会館、大阪
    • Year and Date
      2014-07-22
    • Related Report
      2014 Annual Research Report
    • Invited
  • [Presentation] SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1α,2α,25-, 1α,4α,25- AND 1α,4β,25-TRIHYDROXYVITAMIN D3 WITH METABOLIC STUDIES2014

    • Author(s)
      M. Takano, D. Sawada, K. Yasuda, M. Nishikawa, A. Takeuchi, K. Takagi, K. Horie, G.S. Reddy, T.C. Chen, T. Sakaki, and A. Kittaka
    • Organizer
      17th Vitamin D Workshop
    • Place of Presentation
      Chicago, USA
    • Year and Date
      2014-06-17 – 2014-06-20
    • Related Report
      2014 Annual Research Report
  • [Presentation] 2α位にテトラゾールプロピル基を有する19-ノル型ビタミンD3の合成と生物活性評価2014

    • Author(s)
      高野真史、樋口恵理香、竹内明子、澤田大介、橘高敦史
    • Organizer
      日本ビタミン学会第66回大会
    • Place of Presentation
      姫路商工会議所
    • Year and Date
      2014-06-13 – 2014-06-14
    • Related Report
      2014 Annual Research Report
  • [Presentation] メチルステロール酸化酵素SC4MOLによる2位置換基付加型ビタミンD誘導体の代謝2014

    • Author(s)
      安田佳織、岩永由麻、小川和亮、生城真一、鎌倉昌樹、高野真史、齋藤 望、橘高敦史、藤島利江、太田美穂、榊 利之
    • Organizer
      日本ビタミン学会第66回大会
    • Place of Presentation
      姫路商工会議所
    • Year and Date
      2014-06-13 – 2014-06-14
    • Related Report
      2014 Annual Research Report
  • [Presentation] ビタミンD誘導体設計・合成・生物活性 ~ビタミンD作用の多様性~2014

    • Author(s)
      橘高敦史
    • Organizer
      長崎大学大学院講義(メディシナルケミストリー特論1)
    • Place of Presentation
      長崎大学
    • Year and Date
      2014-05-27
    • Related Report
      2014 Annual Research Report
    • Invited
  • [Presentation] 新規セコステロイド合成と受容体相互作用2014

    • Author(s)
      橘高敦史
    • Organizer
      長崎大学学術講演会
    • Place of Presentation
      長崎大学
    • Year and Date
      2014-05-26
    • Related Report
      2014 Annual Research Report
    • Invited
  • [Presentation] MART-10 Has Enhanced Chemotherapeutic Potency- in vitro and in vivo Pre-clinical Studies2014

    • Author(s)
      K.C. Chiang, A. Kittaka, J.N. Flanagan, T. Sakaki, G. Norstedt and T.C. Chen
    • Organizer
      5th International Symposium Vitamin D and Analogs in Cancer Prevention and Therapy
    • Place of Presentation
      Krefeld, Germany
    • Year and Date
      2014-05-02 – 2014-05-03
    • Related Report
      2014 Annual Research Report
  • [Presentation] Pre-clinical Studies of MART-10, a Less Calcemic Vitamin D Analog, for Cancer Prevention and Treatment2014

    • Author(s)
      Tai C Chen, Kun-Chun Chiang, and Atsushi Kittaka
    • Organizer
      Translational Science 2014 Annual Meeting
    • Place of Presentation
      Omni Shoreham Hotel, Washington DC, USA
    • Year and Date
      2014-04-09 – 2014-04-11
    • Related Report
      2014 Annual Research Report
  • [Presentation] 14-エピ-8,9-ジヒドロ-1α,25-ジヒドロキシ-19-ノルタキステロールの合成2014

    • Author(s)
      澤田大介、松本洋太郎、竹内明子、橘高敦史
    • Organizer
      日本薬学会 第134年会(熊本)
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] 2-[3-(テトラゾール-2-イル)プロピル]-1α,25(OH)2-19-ノルビタミンD3の合成2014

    • Author(s)
      高野真史,樋口恵理香,東 和成,平野圭祐,竹内明子,澤田大介,橘高敦史
    • Organizer
      日本薬学会 第134年会(熊本)
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] 側鎖に金属錯体を持ったβ-PNAによる配列特異的DNA切断2014

    • Author(s)
      杉山 亨、桑田啓子、今村保忠、出水庸介、栗原正明、高野真史、橘高敦史
    • Organizer
      日本薬学会 第134年会(熊本)
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] 14-epi-tachysterol類の合成とVDR結合様式の解明2013

    • Author(s)
      澤田大介、堀江恭平、落合鋭士、竹内明子、角田真二、上村みどり、橘高敦史
    • Organizer
      日本ビタミン学会第65回大会(東京)
    • Place of Presentation
      一橋講堂
    • Related Report
      2013 Research-status Report
  • [Presentation] ビタミンD誘導体設計・合成と初期的生物活性及び制癌活性の新しい知見2013

    • Author(s)
      橘高敦史
    • Organizer
      キッセイ薬品工業株式会社中央研究所・社内講演会
    • Place of Presentation
      キッセイ薬品工業株式会社中央研究所(長野)
    • Related Report
      2013 Research-status Report
    • Invited
  • [Presentation] DESIGN AND SYNTHESIS OF 2α-HETEROARALKYL-1α,25-DIHYDROXYVITAMIN D3 ANALOGS AS STRONG LIGANDS FOR VITAMIN D RECEPTOR2013

    • Author(s)
      M. Matsuo, A. Hasegawa, M. Takano, Y. Nakamura, H. Saitou, S. Kakuda, K. Takagi, E. Ochiai, K. Horie, M. T. Kamimura, K. Takenouchi, D. Sawada, and A. Kittaka
    • Organizer
      16th Vitamin D Workshop(San Francisco, USA)
    • Place of Presentation
      The Palace Hotel
    • Related Report
      2013 Research-status Report
  • [Presentation] Synthesis of 14-Epi-19-Nortachysterol and Elucidation of Its Binding Affinity and Configuration for the Human Vitamin D Receptor2013

    • Author(s)
      D. Sawada, Y. Tsukuda, K. Horie, E. Ochiai, S. Kakuda, M. Takimoto-Kamimura, A. Kittaka
    • Organizer
      14th Tetrahedron Symposium
    • Place of Presentation
      Vienna
    • Related Report
      2013 Research-status Report
  • [Presentation] C5-C6 Coupling of MART-10 Synthesis and Its Clinical Implication in Cancer Treatment and Prevention2013

    • Author(s)
      Masashi Takano, Kun-Chun Chiang, Horng-Heng Juang, Kaori Yasuda, Toshiyuki Sakaki, Toshimasa Itoh, Keiko Yamamoto, Daisuke Sawada, John N. Flanagan, Gunnar Norstedt, Tai C. Chen, and Atsushi Kittaka
    • Organizer
      第10回カルボアニオン化学国際会議(ISCC-10、同志社大学)
    • Place of Presentation
      同志社大学
    • Related Report
      2013 Research-status Report
  • [Presentation] 2α-アゾールエチル基を有する1α,25-ジヒドロキシビタミンD3の合成と生物活性評価2013

    • Author(s)
      橘高敦史、松尾実紀、長谷川麻美、高野真史、澤田大介、齋藤 博、角田真二、高木健一郎、落合鋭士、堀江恭平、上村みどり、竹之内一弥
    • Organizer
      第340回脂溶性ビタミン総合研究委員会(芝浦工大)
    • Place of Presentation
      芝浦工業大学芝キャンパス
    • Related Report
      2013 Research-status Report
  • [Presentation] 7,8-cis-1α,25(OH)2-19-norvitamin D3の合成と活性評価2013

    • Author(s)
      澤田大介、森 幸樹、安部成郁、近藤美保、塩田真由美、竹内明子、橘高敦史
    • Organizer
      第57回日本薬学会関東支部大会(帝京大学)
    • Place of Presentation
      帝京大学板橋キャンパス
    • Related Report
      2013 Research-status Report
  • [Presentation] 2α置換基上にアゾール環を有する19-ノル型ビタミンD3の合成研究2013

    • Author(s)
      樋口恵理香、高野真史、澤田大介、橘高敦史
    • Organizer
      第57回日本薬学会関東支部大会(帝京大学)
    • Place of Presentation
      帝京大学板橋キャンパス
    • Related Report
      2013 Research-status Report
  • [Presentation] ビタミンDとくすり2013

    • Author(s)
      橘高敦史
    • Organizer
      帝京大学公開講座
    • Place of Presentation
      帝京大学板橋キャンパス
    • Related Report
      2013 Research-status Report
    • Invited
  • [Presentation] 7,8-cis-vitamin D3類の合成、活性評価、及びVDR結合様式の解明2013

    • Author(s)
      澤田大介、斎藤博、堀江恭平、高木健一郎、竹内明子、上村みどり、橘高敦史
    • Organizer
      第39回反応と合成の進歩シンポジウム(九州大学)
    • Place of Presentation
      九州大学医学部百年記念講堂
    • Related Report
      2013 Research-status Report
  • [Presentation] Sequence-Specific Cleavage of DNA by a Chiral Peptide Nucleic Acid Bearing a Pendant Metal Complex2013

    • Author(s)
      Toru Sugiyama, Keiko Kuwata, Yasutada Imamura, Yosuke Demizu, Masaaki Kurihara, Masashi Takano, and Atsushi Kittaka
    • Organizer
      第50回ペプチド討論会(大阪)
    • Place of Presentation
      ホテル阪急エキスポパーク
    • Related Report
      2013 Research-status Report
  • [Presentation] 14-epi-tachysterol類の合成、生物活性評価、及び受容体結合様式の解明2013

    • Author(s)
      澤田大介,佃 勇也,堀江恭平,竹内明子,角田真二,上村みどり,橘高敦史
    • Organizer
      第31回メディシナルケミストリーシンポジウム(広島)
    • Place of Presentation
      広島アステールプラザ
    • Related Report
      2013 Research-status Report
  • [Presentation] 7,8-cis-14-epi-19-Norvitamin D3誘導体の合成と活性評価2013

    • Author(s)
      澤田大介ら
    • Organizer
      日本薬学会 第133年会
    • Place of Presentation
      パシフィコ横浜
    • Related Report
      2012 Research-status Report
  • [Presentation] 2α-(3-ヒドロキシプロポキシ)活性型ビタミンD3の代謝物の同定2013

    • Author(s)
      塩谷亜美ら
    • Organizer
      日本薬学会 第133年会
    • Place of Presentation
      パシフィコ横浜
    • Related Report
      2012 Research-status Report
  • [Presentation] β-Lys PNAの合成2013

    • Author(s)
      杉山 亨ら
    • Organizer
      日本薬学会 第133年会
    • Place of Presentation
      パシフィコ横浜
    • Related Report
      2012 Research-status Report
  • [Presentation] REVISITING THE MINOR VITAMIN D FAMILY: A NEW TACHYSTEROL ANALOG AND ITS UNPRESEDENTED BINDING CONFIGURATION FOR THE HUMAN VITAMIN D RECEPTOR2012

    • Author(s)
      Daisuke Sawada et al.
    • Organizer
      15th Vitamin D Workshop
    • Place of Presentation
      Houston Intercontinental Hotel, USA
    • Related Report
      2012 Research-status Report
  • [Presentation] SYNTHESIS OF NOVEL C-2 SUBSTITUTED VITAMIN D DERIVATIVES HAVING RINGED SIDE CHAINS AND THEIR BIOLOGICAL EVALUATION ON BONE2012

    • Author(s)
      Hiroshi Saito et al.
    • Organizer
      15th Vitamin D Workshop
    • Place of Presentation
      Houston Intercontinental Hotel, USA
    • Related Report
      2012 Research-status Report
  • [Presentation] ヒト由来CYP24A1抵抗性ビタミンD誘導体合成とATRA耐性APL細胞分化誘導2012

    • Author(s)
      高野真史ら
    • Organizer
      日本ビタミン学会第64回大会
    • Place of Presentation
      長良川国際会議場
    • Related Report
      2012 Research-status Report
  • [Presentation] 14-epi-19-Nortachysterol as a New Lead Compound in Vitamin D Family and Its Unprecedented Binding Configuration for the Human Vitamin D Receptor2012

    • Author(s)
      Daisuke Sawada et al.
    • Organizer
      XXIInd International Symposium on Medicinal Chemistry (ISMC 2012)
    • Place of Presentation
      Berlin, Germany
    • Related Report
      2012 Research-status Report
  • [Presentation] 2α-(3-ヒドロキシプロピル)-1α,25-ジヒドロキシ-19-ノルビタミンD3(MART-10)とその類縁体の合成と制がん活性等2012

    • Author(s)
      橘高敦史ら
    • Organizer
      第336回脂溶性ビタミン総合研究委員会
    • Place of Presentation
      東京農業大学
    • Related Report
      2012 Research-status Report
  • [Presentation] 2α-ヘテロアラルキル活性型ビタミンD3の合成と生物活性:2α側鎖長の研究2012

    • Author(s)
      高野真史ら
    • Organizer
      第42回複素環化学討論会
    • Place of Presentation
      京都テルサ
    • Related Report
      2012 Research-status Report
  • [Presentation] 優れた医療人の育成と基礎研究の両立を目指して2012

    • Author(s)
      橘高敦史
    • Organizer
      第56回日本薬学会関東支部大会
    • Place of Presentation
      昭和大学
    • Related Report
      2012 Research-status Report
    • Invited
  • [Presentation] 1α,2α,25-トリヒドロキシビタミンD3の合成研究2012

    • Author(s)
      大屋さおり ら
    • Organizer
      第56回日本薬学会関東支部大会
    • Place of Presentation
      昭和大学
    • Related Report
      2012 Research-status Report
  • [Presentation] 14-epi-1α,25-dihydroxytachysterolの合成と生物活性評価2012

    • Author(s)
      澤田大介ら
    • Organizer
      第38回反応と合成の進歩シンポジウム
    • Place of Presentation
      タワーホール船堀
    • Related Report
      2012 Research-status Report
  • [Presentation] SYNTHESIS OF β-CHIRAL PEPTIDE NUCLEIC ACIDS BEARING LYSINE SIDE CHAINS2012

    • Author(s)
      Toru Sugiyama et al.
    • Organizer
      第49回ペプチド討論会
    • Place of Presentation
      かごしま県民交流センター
    • Related Report
      2012 Research-status Report
  • [Presentation] Synthesis Of New C15-Substituted 16-Ene-1α,25-dihydroxyvitamin D3 Analogs and The Receptor-ligand Interaction Studies2012

    • Author(s)
      Atsushi Kittaka et al.
    • Organizer
      13th Tetrahedron Symposium
    • Place of Presentation
      台北
    • Related Report
      2012 Research-status Report
  • [Presentation] 2α-アルコキシ置換活性型ビタミンD3誘導体の代謝と合成研究2012

    • Author(s)
      高野真史ら
    • Organizer
      第30回メディシナルケミストリーシンポジウム
    • Place of Presentation
      タワーホール船堀
    • Related Report
      2012 Research-status Report
  • [Presentation] 長鎖アルキル基を有するノンセコステロイド型VDRリガンドの創製2012

    • Author(s)
      出水庸介ら
    • Organizer
      第30回メディシナルケミストリーシンポジウム
    • Place of Presentation
      タワーホール船堀
    • Related Report
      2012 Research-status Report
  • [Presentation] Synthesis of 1α,2α,25-Trihydroxyvitamin D3: Major Metabolite of 2α-(3-Hydroxypropoxy)-1α,25-dihydroxyvitamin D3 by CYP3A42012

    • Author(s)
      Masashi Takano et al.
    • Organizer
      チトクロームP450発見50周年記念シンポジウム
    • Place of Presentation
      九州大学医学部コラボレーション
    • Related Report
      2012 Research-status Report
  • [Book] スタンダード薬学シリーズⅡ 3 化学系薬学Ⅰ.「化学物質の性質と反応」2015

    • Author(s)
      橘高敦史 領域担当編集
    • Total Pages
      445
    • Publisher
      東京化学同人
    • Related Report
      2014 Annual Research Report
  • [Book] ビタミンDと疾患~基礎の理解と臨床への応用~2014

    • Author(s)
      岡野登志夫編、橘高敦史共著
    • Total Pages
      246
    • Publisher
      医薬ジャーナル社(大阪)
    • Related Report
      2013 Research-status Report
  • [Remarks] 橘高敦史

    • URL

      http://researchmap.jp/read0025684/

    • Related Report
      2014 Annual Research Report
  • [Remarks] 薬化学研究室

    • URL

      http://www.pharm.teikyo-u.ac.jp/

    • Related Report
      2014 Annual Research Report
  • [Remarks] 帝京大学薬学部・医薬化学講座・薬化学研究室

    • URL

      http://www.e-campus.gr.jp/staffinfo/public/staff/detail/419/16

    • Related Report
      2013 Research-status Report
  • [Remarks] 帝京大学薬学部・医薬化学講座・薬化学研究室

    • URL

      http://www.pharm.teikyo-u.ac.jp/

    • Related Report
      2013 Research-status Report
  • [Remarks] 帝京大学薬学部・医薬化学講座・薬化学研究室

    • URL

      http://www.e-campus.gr.jp/staffinfo/public/staff/detail/419/16

    • Related Report
      2012 Research-status Report
  • [Remarks] 帝京大学薬学部・医薬化学講座・薬化学研究室

    • URL

      http://www.pharm.teikyo-u.ac.jp/lab/yakka/index.html

    • Related Report
      2012 Research-status Report

URL: 

Published: 2013-05-31   Modified: 2019-07-29  

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