14-epi-Previtamin D Analogs : Design and Synthesis of Selective Ligands for Nuclear Receptor and Membrane Receptor
| Project/Area Number |
19590016
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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 |
KITTAKA Atsushi Teikyo University, 薬学部, 教授 (00214833)
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| Co-Investigator(Kenkyū-buntansha) |
SAWADA Daisuke 帝京大学, 薬学部, 講師 (00338691)
TAKANO Masashi 帝京大学, 薬学部, 助教 (50386611)
SUGIYAMA Toru 東京大学, 大学院・総合文化研究科, 助教 (40242036)
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| Project Period (FY) |
2007 – 2008
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| Project Status |
Completed (Fiscal Year 2008)
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| Budget Amount *help |
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2008: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2007: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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| Keywords | 生体関連物質 / ビタミンD受容体 / 活性型ビタミンD_3 / 14-エピ-プレビタミンD_3 / オステオカルシン / 転写活性 / 骨芽細胞 / [1,7]シグマトロピー転位 / ビタミンD受容体(VDR) / プレビタミンD_3 / ルミステロール / genomic作用 / nongenomic作用 / 14-エピー活性型ビタミンD_3 / 活性型ビタミンD / 14-エピ-活性型ビタミンD_3 |
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| Research Abstract |
活性型ビタミンD_3(1)は、生体内で異性体プレビタミンD_3(2)との平衡混合物(37℃溶液中で1 : 2 = 94 : 6)として存在する。核内受容体に結合する1と異なり2の生理作用については不明な点が多く、細胞膜上に2 の受容体が想定されている。化学平衡で1へと容易に異性化する2の構造を固定化するために14位のエピ化を施し、次いで2 位の化学修飾、さらに19 位のノル化を検討したところ、新規化合物として天然ホルモン1を超える骨芽細胞(HOS)における骨形成増強作用を見出した。
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Report
(3 results)
Research Products
(132 results)
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[Journal Article] (2 S,2' R)-Analogue of LG190178 Is a Major Active Isomer2008
Author(s)
Wataru Hakamata, Yukiko Sato, Haruhiro Okuda, Shinobu Honzawa, Nozomi Saito, Seishi Kishimoto, Atsushi Yamashita, Takayuki Sugiura, Atsushi Kittaka, Masaaki Kurihara
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Journal Title
Bioorg. Med. Chem. Lett 18
Pages: 120-123
Related Report
Peer Reviewed
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[Journal Article] Kinetic Studies of 25-Hydroxy-19-Nor-Vitamin D_3 and 1α,25-Dihydroxy-19-Nor-Vitamin D_3 Hydroxylation by CYP27B1 and CYP24A12007
Author(s)
Naoko Urushino, Sachie Nakabayashi, Midori A. Arai, Atsushi Kittaka, Tai C. Chen, Keiko Yamamoto, Keiko Hayashi, Shigeaki Kato, Miho Ohta, Masaki Kamakura, Shinichi Ikushiro, Toshiyuki Sakaki
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Journal Title
Drug Metab. Dispos. 35
Pages: 1482-1488
Related Report
Peer Reviewed
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[Journal Article] Synthesis and Biologica Activities of 14- epi-MART-10 and 14- epi-MART-11 : Implications for Cancer and Osteoporosis Treatment
Author(s)
Atsushi Kittaka, Hideki Hara, Masashi Takano, Daisuke Sawada, Midori A. Arai, Kenichiro Takagi, Takayuki Chida, Yoshifumi Harada, Hiroshi Saito, Kazuya Takenouchi, Seiichi Ishizuka, Keiko Hayashi, Shinichi Ikushiro, Toshiyuki Sakaki, Takayuki Sugiura, Tai C. Chen
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Journal Title
Anticancer Res.(in press)
Related Report
Peer Reviewed
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[Journal Article] Evaluation of 19-nor-2α-(3-hydroxypropyl)-1α,25-dihydroxyvitamin D_3 As a Therapeutic Agent for Androgen-dependent Prostate Cancer
Author(s)
John N. Flanagan, Shasha Zheng, Kun-Chun Chiang, Atsushi Kittaka, Toshiyuki Sakaki, Sachie akabayashi, Remco A. Spanjaard, Kelly S. Persons, Jeffrey S. athieu, Michael F. Holick, Tai C. Chen
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Journal Title
Anticancer Res.(in press)
Related Report
Peer Reviewed
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[Presentation] New Vitamin D_3 Analogs : 2α-(2,3-Dihydroxypropoxy)-and 2α-(2-Hydroxypropoxy)- Active Vitamin D_3 with Highly Potent VDR Agonism2008
Author(s)
Masashi Takano, Daisuke Sawada, Keiko Hayashi, Shin-ichi Ikushiro, Toshiyuki Sakaki, Ken-ichiro Takagi, Seiichi Ishizuka, Midori Takimoto-Kamimura, Maiko Gokoh, Takayuki Sugiura, Atsushi Kittaka
Organizer
第236回アメリカ化学会
Place of Presentation
Philadelphia, USA
Related Report
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[Presentation] Synthesis and Biological Evaluation of Novel 2-Substituted 14- epi-Previtamin D_3 Analogs2008
Author(s)
Daisuke Sawada, Yuya Tsukuda, Nozomi Saito, Tomoyuki Katayama, Hiroshi Saito, Ken-ichiro Takagi, Kazuya Takenouchi, Seiichi Ishizuka, Midori Takimoto-Kamimura, Masashi Takano, Atsushi Kittaka
Organizer
第236回アメリカ化学会
Place of Presentation
Philadelphia, USA
Related Report
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[Presentation] Structure-Activity Relationship Study on Vitamin D Receptor Antagonist TEI-9647 Analogs2008
Author(s)
Nozomi Saito, Manami Masuda, Toshihiro Matsunaga, Hiroshi Saito, Miyuki Anzai, Kazuya Takenouchi, Daishiro Miura, Jun-ichi Namekawa, Seiichi Ishizuka, Midori Takimoto-Kamimura, Atsushi Kittaka
Organizer
第236回アメリカ化学会
Place of Presentation
Philadelphia, USA
Related Report
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[Presentation] Vitamin D hormone : structural refinement of the secosteroidal skeleton and the nuclear receptor mediated biological activity2008
Author(s)
Atsushi Kittaka, Daisuke Sawada, Masashi Takano, Nozomi Saito, Tomoyuki Katayama, Kanako Shindo, Yuya Tsukuda, Shinobu Honzawa, Midori A. Arai, Hiroshi Saito, Ken-ichiro Takagi, Kazuya Takenouchi, Seiichi Ishizuka, Toshiyuki Sakaki, and Tai C. Chen
Organizer
3rd Symposium Vitamin D Analogs in Cancer Prevention and Therapy
Place of Presentation
Krefeld, Germany
Related Report
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[Presentation] Synthesis of New 14- epi-Previtamin D_3 Analogs : Effect of C2-Modification on Biological Activity(Brown University Vitamin D Research Award 受賞発表)2007
Author(s)
Daisuke Sawada, Nozomi Saito, Tomoyuki Katayama, Yuya Tsukuda, Masashi Takano, Hiroshi Saito, Ken-ichiro Takagi, Kazuya Takenouchi, Seiichi Ishizuka, Midori Takimoto-Kamimura, Atsushi Kittaka
Organizer
The 14th Annual Providence Symposium on Vitamin D
Place of Presentation
Brown University
Related Report
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