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2011 Fiscal Year Final Research Report

Efficient Creation of Drug-functional Molecules with Chemically Evolutional Synthetic Chemistry

Research Project

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Project/Area Number 20249006
Research Category

Grant-in-Aid for Scientific Research (A)

Allocation TypeSingle-year Grants
Section一般
Research Field Drug development chemistry
Research InstitutionNagoya City University

Principal Investigator

HIGUCHI Tsunehiko  名古屋市立大学, 大学院・薬学研究科, 教授 (50173159)

Co-Investigator(Kenkyū-buntansha) UMEZAWA Naoki  名古屋市立大学, 大学院・薬学研究科, 准教授 (40347422)
KATO Nobuki  名古屋市立大学, 大学院・薬学研究科, 助教 (50400221)
Co-Investigator(Renkei-kenkyūsha) IMAIZUMI Yuji  名古屋市立大学, 大学院・薬学研究科, 教授 (60117794)
Project Period (FY) 2008 – 2011
Keywords化学平衡 / 親和性 / ダイナミックコンビナトリアルケミストリー / 創薬手法
Research Abstract

We have succeeded in the development of 2, 4, 6-triethyl-1, 3, 5-di(alkylamino) benzene dynamic combinatorial library having affinity to hemin by utilizing aldehyde/amine-imine equilibrium reaction between 2, 4, 6-triethyl-1, 3, 5-benzenetricarbaldehyde(1) scaffold and amines. Increased products in the presence of hemin had higher affinity with hemin than not increased products. Porphyrin having four aldehyde precursors as a scaffold was synthesized. Equilibrium reaction between scaffold 1 and boomerang-form diamines converged to a cage-type supramolecule mainly.

  • Research Products

    (20 results)

All 2011 2010 2009 2008 Other

All Journal Article (10 results) (of which Peer Reviewed: 9 results) Presentation (4 results) Book (1 results) Remarks (1 results) Patent(Industrial Property Rights) (4 results) (of which Overseas: 1 results)

  • [Journal Article] Photocontrol of Peptide Function : Backbone Cyclization Strategy with Photocleavable Amino Acid2011

    • Author(s)
      Naoki Umezawa, Yuka Noro, Kazuhiro Ukai, Nobuki Kato, Tsunehiko Higuchi
    • Journal Title

      Chem. Bio. Chem.

      Volume: 12(13) Pages: 1694-1698

    • DOI

      DOI:10.1002/cbic.201100212

    • Peer Reviewed
  • [Journal Article] Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM12010

    • Author(s)
      Shinya Mimasu, Naoki Umezawa, Shin Sato, Tsunehiko Higuchi, Takashi Umehara, and Shigeyuki Yokoyama
    • Journal Title

      Biochemistry

      Volume: 49(30) Pages: 6494-6503

    • Peer Reviewed
  • [Journal Article] Facile synthesis of peptide-porphyrin conjugates : Towards artificial catalase2010

    • Author(s)
      Naoki Umezawa, Nobuyoshi Matsumoto, Shinsuke Iwama, Nobuki Kato and Tsunehiko Higuchi
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 18(17) Pages: 6340-6350

    • Peer Reviewed
  • [Journal Article] Turn-on fluorescent probe with visible light excitation for labeling of hexahistidine tagged protein2009

    • Author(s)
      Mie Kamoto, Naoki Umezawa, Nobuki Kato, and Tsunehiko Higuchi
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 19(8) Pages: 2285-2288

    • Peer Reviewed
  • [Journal Article] Inhibition ofγ-Secretase Activity by Helicalβ-Peptide Foldamers2009

    • Author(s)
      Yuki Imamura, Naoto Watanabe, Naoki Umezawa, Takeshi Iwatsubo, Nobuki Kato, Taisuke Tomita, and Tsunehiko Higuchi
    • Journal Title

      J. Am. Chem. Soc.

      Volume: 131(21) Pages: 7353-7359

    • Peer Reviewed
  • [Journal Article] Spectroscopic and Mechanistic Studies on Oxidation Reactions Catalyzed by the Functional Model SR Complex for Cytochrome P450 : Influence of Oxidant, Substrate, and Solvent2009

    • Author(s)
      Natalya Hessenauer-Ilicheva, Alicja Franke, Maria Wolak, Tsunehiko Higuchi, and Rudi van Eldik
    • Journal Title

      Chem. Eur. J.

      Volume: 15(45) Pages: 12447-12459

    • Peer Reviewed
  • [Journal Article] 触媒機能におけるシトクロムP450配位構造の必然性:モデル錯体からのアプローチ2009

    • Author(s)
      樋口恒彦
    • Journal Title

      有機合成化学協会誌

      Volume: 67(2) Pages: 134-142

  • [Journal Article] Extreme rate acceleration by axial thiolate coordination on the isomerization of endoperoxide catalyzed by iron porphyrin : relevance to prostaglandin H2 isomerase catalysis2008

    • Author(s)
      Takehiro Yamane, Kohei Makino, Naoki Umezawa, Nobuki Kato, and Tsunehiko Higuchi
    • Journal Title

      Angew. Chem. Int. Ed.

      Volume: 47(34) Pages: 6438-6440

    • Peer Reviewed
  • [Journal Article] Novel Probes Showing Specific Fluorescence Enhancement on Binding to Hexahistidine Tag2008

    • Author(s)
      Mie Kamoto, Naoki Umezawa, Nobuki Kato, and Tsunehiko Higuchi
    • Journal Title

      Chem.-Eur. J.

      Volume: 14(26) Pages: 8004-8012

    • Peer Reviewed
  • [Journal Article] Array-based fluorescence assay for serine/threonine kinases using specific chemical reaction2008

    • Author(s)
      Shoji Akita, Naoki Umezawa, Nobuki Kato, and Tsunehiko Higuchi
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 16(16) Pages: 7788-7794

    • Peer Reviewed
  • [Presentation] 化学進化的合成化学:新規スカッフォルドの合成とアミロイドβ親和性分子創製の検討2011

    • Author(s)
      串田優, 加藤信樹, 梅澤直樹, 樋口恒彦
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Year and Date
      2011-03-29
  • [Presentation] 化学進化的合成化学による抗マラリア薬を目指した高ヘム親和性化合物の開発2009

    • Author(s)
      藪名香宏介, 梅澤直樹, 加藤信樹, 樋口恒彦
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      京都
    • Year and Date
      2009-03-28
  • [Presentation] 化学進化的合成化学による抗マラリア薬を目指した高ヘム親和性化合物の開発2008

    • Author(s)
      藪名香宏介, 梅澤直樹, 加藤信樹, 樋口恒彦
    • Organizer
      第27回メディシナルケミストリーシンポジウム
    • Place of Presentation
      大阪
    • Year and Date
      2008-11-27
  • [Presentation] 官能基集積型機能分子:酵素機構解明から医薬候補分子創製まで2008

    • Author(s)
      樋口恒彦
    • Organizer
      京都大学大学院薬学研究科
    • Place of Presentation
      京都
    • Year and Date
      2008-10-15
  • [Book] 無機化学

    • Author(s)
      樋口恒彦
    • Publisher
      株式会社化学同人
  • [Remarks]

    • URL

      http://www.phar.nagoya-cu.ac.jp/hp/ysk/index.html

  • [Patent(Industrial Property Rights)] 抗マラリア活性化合物及び抗マラリア薬2011

    • Inventor(s)
      樋口恒彦、梅澤直樹、加藤信樹
    • Industrial Property Rights Holder
      名古屋市立大学/(株)セラバリューズ
    • Industrial Property Number
      特許、PCT/JP2011/069392
    • Filing Date
      2011-08-29
    • Overseas
  • [Patent(Industrial Property Rights)] 抗マラリア活性化合物及び抗マラリア薬2010

    • Inventor(s)
      樋口恒彦、梅澤直樹、加藤信樹
    • Industrial Property Rights Holder
      名古屋市立大学/(株)セラバリューズ
    • Industrial Property Number
      特許、特願2010-198651
    • Filing Date
      2010-09-06
  • [Patent(Industrial Property Rights)] ケージド化合物の製造方法2008

    • Inventor(s)
      梅澤直樹、鵜飼和宏、樋口恒彦
    • Industrial Property Rights Holder
      名古屋市立大学
    • Industrial Property Number
      特許、特願2008-16771
    • Filing Date
      2008-06-26
  • [Patent(Industrial Property Rights)] 核酸複合体2008

    • Inventor(s)
      筒井宏典、渡邉健太郎、山本勝也、樋口恒彦、松本春香、加藤信樹、梅澤直樹
    • Industrial Property Rights Holder
      日産自動車(株)/名古屋市立大学
    • Industrial Property Number
      特許、特願2008-59853
    • Filing Date
      2008-03-10

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Published: 2013-07-31  

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