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Development of molecular probes for steroid hormone receptor functions

Research Project

Project/Area Number 24590137
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionOchanomizu University

Principal Investigator

TANATANI Aya  お茶の水女子大学, 大学院人間文化創成科学研究科, 准教授 (40361654)

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: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsステロイドホルモン / 核内受容体 / アンドロゲン / プロゲステロン / アンタゴニスト / 蛍光性リガンド / クマリン / 光学分割 / 蛍光プローブ / フタラジノン
Outline of Final Research Achievements

In this study, the specific ligands and fluorescence probes for steroid hormone nuclear receptors were developed.
(1) Phthalazinone derivatives were developed as novel androgen antagonists, and acted as antagonists towards both wild-type and mutated ARs. As progesterone antagonists, compounds bearing a carborane or adamantane as the hydrophobic pharmacophore were developed.
(2) Coumarine derivatives were developed as fluorescent progesterone antagonists, whose fluorescence intensity was strongly increased by binding to progesterone receptor. Coumarine derivatives with androgen antagonistic activity were also developed.

Report

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

    (46 results)

All 2015 2014 2013 2012

All Journal Article (14 results) (of which Peer Reviewed: 14 results,  Acknowledgement Compliant: 3 results) Presentation (32 results)

  • [Journal Article] Development of 1,3-diphenyladamantane derivatives as nonsteroidal progesterone receptor antagonists.2015

    • Author(s)
      Mori, S.; Takeuchi, Y.; Tanatani, A.; Kagechika, H.; Fujii, S.
    • Journal Title

      Bioorg. Med. Chem

      Volume: 23 Issue: 4 Pages: 803-809

    • DOI

      10.1016/j.bmc.2014.12.047

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Structural Characterization of Partly-Folded Foldamers with No Long Range Conformational Order.2014

    • Author(s)
      Kudo, M.; Maurizot, V.; Masu, H.; Tanatani, A.; and Huc, I.
    • Journal Title

      Chem. Comm.

      Volume: 50 Issue: 70 Pages: 10090-10093

    • DOI

      10.1039/c4cc03822c

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Design and synthesis of tetraol derivatives of 1,12-dicarba-closo-dodecaborane as non-secosteroidal vitamin D analogs.2014

    • Author(s)
      Fujii, S.; Kano, A.; Masuno, H.; Songkram, C.; Kawachi, E.; Hirano, T.; Tanatani, A.; Kagechika, H
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 24 Issue: 18 Pages: 4515-4519

    • DOI

      10.1016/j.bmcl.2014.07.075

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Structural development of p-carborane-based potent non-secosteroidal vitamin D analogs.2014

    • Author(s)
      Fujii, S.; Sekine, R.; Kano, A.; Masuno, H.; Songkram, C.; Kawachi, E.; Hirano, T.; Tanatani, A.; Kagechika, H.
    • Journal Title

      Bioorg. Med. Chem

      Volume: 22 Issue: 21 Pages: 5891-5901

    • DOI

      10.1016/j.bmc.2014.09.020

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Lipase-catalyzed asymmetric acylation of boron cluster-containing secondary alcohols.2014

    • Author(s)
      Mori, S.; Takagaki, R.; Fujii, S.; Matsumura, M.; Tanatani, A.; Kagechika, H.
    • Journal Title

      Tetrahedron Asymm.

      Volume: 25 Issue: 23 Pages: 1505-1512

    • DOI

      10.1016/j.tetasy.2014.10.009

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Synthesis and structure-activity relationship of p-carborane-based non-secosteroidal vitamin D analogs.2014

    • Author(s)
      Fujii, S.; Kano, A.; Songkram, C.; Masuno, H.; Tao da, Y.; Kawachi, E.; Hirano, T.; Tanatani, A.; Kagechika, H.
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 22 Issue: 4 Pages: 1227-1235

    • DOI

      10.1016/j.bmc.2014.01.015

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Folding of a Linear Array of α-Amino Acids within a Helical Aromatic Oligoamide Frame2013

    • Author(s)
      Mayumi Kudo, Victor Maurizot, Brice Kauffmann, Aya Tanatani, and Ivan Huc
    • Journal Title

      J. Am. Chem. Soc.

      Volume: 135 Issue: 26 Pages: 9628-9631

    • DOI

      10.1021/ja404656z

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis of Porphyrinylamide and Observation of N-Methylation-induced trans-cis Amide Conformational Alteration2013

    • Author(s)
      Matsumura, M.; Aya Tanatani; Kaneko, T.; Azumaya, I.; Masu, H.; Hashizume, D.; Kagechika, H.; Muranaka, A.; Uchiyama, M.
    • Journal Title

      Tetrahedron

      Volume: 69 Issue: 51 Pages: 10927-10932

    • DOI

      10.1016/j.tet.2013.10.069

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Unusual Conformational Preference of an Aromatic Secondary Urea:Solvent-dependent Open-Closed Conformational Switching of N,N’-Bis(porphyrinyl)urea2013

    • Author(s)
      Matsumura, M.
    • Journal Title

      Chem. Comm.

      Volume: 49 Issue: 23 Pages: 2290-2292

    • DOI

      10.1039/c2cc37583d

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Redox-Responsive Conformational Alteration of Aromatic Amides Bearing N-Quinonyl System2012

    • Author(s)
      Iwao Okamoto, Yusuke Takahashi, Mika Sawamura, Mio Matsumura, Hyuma Masu, Kosuke Katagiri, Isao Azumaya, Masanori Nishino, Yukari Kohama, Nobuyoshi Morita, Osamu Tamura, Hiroyuki Kagechika, Aya Tanatani
    • Journal Title

      Tetrahedron

      Volume: 68 Issue: 27-28 Pages: 5346-5355

    • DOI

      10.1016/j.tet.2012.04.114

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Molecular Chirality and Chiral Capsule-type Dimer Formation of Cyclic Triamides via Hydrogen-Bonding Interactions2012

    • Author(s)
      Fujimoto, N.
    • Journal Title

      Chem. Commun.

      Volume: 48 Issue: 40 Pages: 4809-4811

    • DOI

      10.1039/c2cc18177k

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis and Helical Properties of Aromatic Multilayered Oligoureas2012

    • Author(s)
      Kudo, M.
    • Journal Title

      Tetrahedron

      Volume: 68 Issue: 23 Pages: 4455-4463

    • DOI

      10.1016/j.tet.2011.12.038

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Solvent-dependent Conformational and Fluorescence Change of an N-Phenylbenzohydroxamic Acid Derivative Bearing Two Pyrene Moieties.2012

    • Author(s)
      Misae Kanai, Tomoya Hirano, Isao Azumaya, Iwao Okamoto, Hiroyuki Kagechika, Aya Tanatani
    • Journal Title

      Tetrahedron

      Volume: 68 Issue: 13 Pages: 2778-2783

    • DOI

      10.1016/j.tet.2012.02.012

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Novel vitamin D receptor ligands bearing a spherical hydrophobic core structure-Comparison of bicyclic hydrocarbon derivatives with boron cluster derivatives2012

    • Author(s)
      Wongmayura, A.
    • Journal Title

      Bioorg.Med Chem.Lett.

      Volume: 22 Issue: 4 Pages: 1756-1760

    • DOI

      10.1016/j.bmcl.2011.12.137

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Presentation] カルボラン含有プロゲステロン受容体リガンドのリパーゼによる光学分割2015

    • Author(s)
      森修一、高垣亮平、藤井晋也、松村実生、棚谷綾、影近弘之
    • Organizer
      日本薬学会第135年会
    • Place of Presentation
      神戸
    • Year and Date
      2015-03-26 – 2015-03-28
    • Related Report
      2014 Annual Research Report
  • [Presentation] Lipase-catalyzed asymmetric acylation of boron cluster-containing secondary alcohols2014

    • Author(s)
      Shuichi Mori, Ryohei Takagaki, Shinya Fujii, Mio Matsumura, Aya Tanatani, and Hiroyuki Kagechika
    • Organizer
      Active Enzyme Molecule 2014
    • Place of Presentation
      富山
    • Year and Date
      2014-12-17 – 2014-12-19
    • Related Report
      2014 Annual Research Report
  • [Presentation] クマリン骨格を基盤としたアンドロゲンアンタゴニストの創製研究2014

    • Author(s)
      古賀瞳、木下満里絵、藤井晋也、影近弘之、棚谷綾
    • 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
    • Year and Date
      2014-11-26 – 2014-11-28
    • Related Report
      2014 Annual Research Report
  • [Presentation] Lipase-catalyzed optical resolution and biological activity of boron-cluster-based progesterone receptor ligands2014

    • Author(s)
      Shuichi Mori, Ryohei Takagaki, Shinya Fujii, Mio Matsumura, Aya Tanatani, Hiroyuki Kagechika
    • Organizer
      3rd International Chemical Biology Meeting
    • Place of Presentation
      San Fracisco, USA
    • Year and Date
      2014-11-17 – 2014-11-20
    • Related Report
      2014 Annual Research Report
  • [Presentation] 新規7-アミドクマリン誘導体のアンドロゲンアンタゴニスト活性2014

    • Author(s)
      古賀瞳、木下満里絵、藤井晋也、影近弘之、棚谷綾
    • Organizer
      日本レチノイド研究会第25回学術集会
    • Place of Presentation
      秋田
    • Year and Date
      2014-10-08 – 2014-10-09
    • Related Report
      2014 Annual Research Report
  • [Presentation] Formation of Helical Structures of N,N’-Bis(ortho-substituted phenyl)squaramides in the Crystals2014

    • Author(s)
      Aya Tanatani, Midori Kanda, Shinya Fujii, Mio Matsumura, Kosuke Katagiri, Hyuma Masu, Isao Azumaya, Hiroyuki Kagechika
    • Organizer
      Joint congress of Asian Crystallization Technology Symposium-2014 and11th International Workshop on Crystal Growth of Organic Materials
    • Place of Presentation
      奈良
    • Year and Date
      2014-06-17 – 2014-06-20
    • Related Report
      2014 Annual Research Report
  • [Presentation] Crystal structure of the aromatic helical molecule with hydrogen bond ability on the surface2014

    • Author(s)
      Misae Kanai, Victor Maurizot, Hyuma Masu, Aya Tanatani, Ivan Huc
    • Organizer
      Joint congress of Asian Crystallization Technology Symposium-2014 and11th International Workshop on Crystal Growth of Organic Materials
    • Place of Presentation
      奈良
    • Year and Date
      2014-06-17 – 2014-06-20
    • Related Report
      2014 Annual Research Report
  • [Presentation] クマリン骨格を基盤とした新規アンドロゲン受容体アンタゴニストの創製2014

    • Author(s)
      古賀瞳、木下満里絵、藤井晋也、影近弘之、棚谷綾
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本大学(熊本)
    • Related Report
      2013 Research-status Report
  • [Presentation] Aromatic Foldamers Based on the Cis Conformational Preference of N-Alkylated Aromatic Amide and Urea Bonds2013

    • Author(s)
      Aya Tanatani, Mayumi Kudo, Mio Matsumura, Yukiko Tojo, Tomoyo Kaneko, Shizuka Nishiyama, Hyuma Masu, Isao Azumaya, Hiroyuki Kagechika
    • Organizer
      PARIS 2013 FOLDAMERS SYMPOSIUM
    • Place of Presentation
      Paris, France
    • Related Report
      2013 Research-status Report
  • [Presentation] N,N’-ビス(オルト置換フェニル)スクアルアミドのらせん形成2013

    • Author(s)
      神田翠、藤井晋也、松村実生、片桐幸輔、桝飛雄馬、東屋功、影近弘之、棚谷綾
    • Organizer
      モレキュラー・キラリティー2013
    • Place of Presentation
      京都大学
    • Related Report
      2013 Research-status Report
  • [Presentation] 光学活性な置換基を導入したピロール含有オリゴアミドの立体挙動2013

    • Author(s)
      東條有希子,工藤まゆみ,松村実生,棚谷綾
    • Organizer
      モレキュラー・キラリティー2013
    • Place of Presentation
      京都大学
    • Related Report
      2013 Research-status Report
  • [Presentation] The conformational and fluorescence change of an N-phenylbenzohydroxamic acid derivative depending on the solvent properties2013

    • Author(s)
      Misae Kanai, Tomoya Hirano, Isao Azumaya, Iwao Okamoto, Hiroyuki Kagechika, Aya Tanatani
    • Organizer
      ISMSC-8
    • Place of Presentation
      Arlinton, VA, USA
    • Related Report
      2013 Research-status Report
  • [Presentation] Formation of Chiral Helical Chain Structures of N,N’-bis(ortho-substituted phenyl)squaramides in the Crystals2013

    • Author(s)
      Midori Kanda, Shinya Fujii, Mio Matsumura, Kosuke Katagiri, Hyuma Masu, Isao Azumaya, Hiroyuki Kagechika, Aya Tanatani
    • Organizer
      ISMSC-8
    • Place of Presentation
      Arlinton, VA, USA
    • Related Report
      2013 Research-status Report
  • [Presentation] 水素結合能性官能基を有する芳香族環状トリアミドの立体挙動2013

    • Author(s)
      西山しずか、松村実生、藤本慎子、桝飛雄真、東屋功、影近弘之、棚谷綾
    • Organizer
      第24回基礎有機化学討論会
    • Place of Presentation
      学習院大学(東京)
    • Related Report
      2013 Research-status Report
  • [Presentation] 亜鉛ポルフィリニルアミドおよびウレアの立体転換2013

    • Author(s)
      金子知世、松村実生、 村中厚哉、内山真伸、影近弘之、棚谷綾
    • Organizer
      第24回基礎有機化学討論会
    • Place of Presentation
      学習院大学(東京)
    • Related Report
      2013 Research-status Report
  • [Presentation] N-メチルピロールを有するN-アルキル化アミドオリゴマーの立体構造解析2013

    • Author(s)
      東條有希子、工藤まゆみ、松村実生、棚谷綾
    • Organizer
      第24回基礎有機化学討論会
    • Place of Presentation
      学習院大学(東京)
    • Related Report
      2013 Research-status Report
  • [Presentation] Cis Conformational Preference of N-Alkylated Aromatic Amide and Urea Bonds: Construction of Aromatic Foldamers with Unique Structures2013

    • Author(s)
      AyTanatani, Isao Azumayaa, Hiroyuki Kagechika
    • Organizer
      ACS National Meeting
    • Place of Presentation
      Indianapolis, USA
    • Related Report
      2013 Research-status Report
  • [Presentation] アンドロゲン受容体アンタゴニスト活性を有する新規フェノキシフェノール誘導体の構造活性相関2013

    • Author(s)
      数井優子、山田歩、藤井晋也、影近弘之、棚谷綾
    • Organizer
      第31回メディシナルケミストリーシンポジウム
    • Place of Presentation
      アステールプラザ(広島)
    • Related Report
      2013 Research-status Report
  • [Presentation] 疎水性球状分子を骨格とする新規PRアンタゴニストの創製2013

    • Author(s)
      竹内由起
    • Organizer
      第133回日本薬学会年会
    • Place of Presentation
      横浜
    • Related Report
      2012 Research-status Report
  • [Presentation] ニッケルポルフィリルウレアオリゴマーの合成とその立体構造解析2013

    • Author(s)
      松村実生
    • Organizer
      日本化学会第93春季年会
    • Place of Presentation
      滋賀
    • Related Report
      2012 Research-status Report
  • [Presentation] 水素結合性官能基を導入した芳香族環状トリアミドの立体特性と分子不斉2013

    • Author(s)
      西山しずか
    • Organizer
      日本化学会第93春季年会
    • Place of Presentation
      滋賀
    • Related Report
      2012 Research-status Report
  • [Presentation] ピロール環含有芳香族オリゴアミドの合成と立体構造解析2013

    • Author(s)
      東條有希子
    • Organizer
      日本化学会第93春季年会
    • Place of Presentation
      滋賀
    • Related Report
      2012 Research-status Report
  • [Presentation] 亜鉛ポルフィリンアミドおよびウレアの合成と立体構造解析2013

    • Author(s)
      金子知世
    • Organizer
      日本化学会第93春季年会
    • Place of Presentation
      滋賀
    • Related Report
      2012 Research-status Report
  • [Presentation] ロイシンまたはオキサゾールを導入したキノリンオリゴアミドフォルダマーの創製2013

    • Author(s)
      工藤まゆみ
    • Organizer
      日本化学会第93春季年会
    • Place of Presentation
      滋賀
    • Related Report
      2012 Research-status Report
  • [Presentation] N,N’-ジアリールスクアルアミドのらせん形成と自然分晶2012

    • Author(s)
      神田翠
    • Organizer
      Molecular Chirality Asia 2012
    • Place of Presentation
      福岡
    • Related Report
      2012 Research-status Report
  • [Presentation] 芳香族環状トリアミドの分子不斉と不斉誘導2012

    • Author(s)
      西山しずか
    • Organizer
      Molecular Chirality Asia 2012
    • Place of Presentation
      福岡
    • Related Report
      2012 Research-status Report
  • [Presentation] アミノ酸分子を組み込んだキノリン骨格を有するフォルダマーの合成と構造解析2012

    • Author(s)
      工藤まゆみ
    • Organizer
      Molecular Chirality Asia 2012
    • Place of Presentation
      福岡
    • Related Report
      2012 Research-status Report
  • [Presentation] カルボラン含有VDRリガンドの構造活性相関と結合様式2012

    • Author(s)
      藤井晋也
    • Organizer
      Molecular Chirality Asia 2012
    • Place of Presentation
      福岡
    • Related Report
      2012 Research-status Report
  • [Presentation] N, N’-ビス(オクタエチルポルフィリニル)ウレア及びそのオリゴマーの合成と立体構造解析2012

    • Author(s)
      松村実生
    • Organizer
      第23回基礎有機化学討論会
    • Place of Presentation
      京都
    • Related Report
      2012 Research-status Report
  • [Presentation] Synthesis and conformational analysis of functional foldamers consisnting of quinoline and natural amino acid2012

    • Author(s)
      Kudo, M.
    • Organizer
      13th Tetrahedron Symposium Asia
    • Place of Presentation
      Taipei, Taiwan
    • Related Report
      2012 Research-status Report
  • [Presentation] Synthesis and conformational properties of N, N’-bis(octaethylporphyrinyl)ureas2012

    • Author(s)
      Matsumura, M.
    • Organizer
      13th Tetrahedron Symposium Asia
    • Place of Presentation
      Taipei, Taiwan
    • Related Report
      2012 Research-status Report
  • [Presentation] 新規6-アリールクマリン誘導体のプロゲステロンアンタゴニスト活性と蛍光特性2012

    • Author(s)
      木下満里絵
    • 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
      船堀
    • Related Report
      2012 Research-status Report

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

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