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2011 Fiscal Year Final Research Report

Development of drug candidates that epigenetically regulate gene expression

Research Project

  • PDF
Project/Area Number 20390034
Research Category

Grant-in-Aid for Scientific Research (B)

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

Principal Investigator

MIYATA Naoki  名古屋市立大学, 大学院・薬学研究科, 教授 (50114674)

Co-Investigator(Renkei-kenkyūsha) SUZUKI Takayoshi  名古屋市立大学, 大学院・薬学研究科, 講師 (90372838)
NAKAGAWA Hidehiko  名古屋市立大学, 大学院・薬学研究科, 准教授 (80281674)
Project Period (FY) 2008 – 2011
Keywordsエピジェネティクス / 遺伝子発現制御 / 創薬分子設計 / ヒストン脱メチル化酵素阻害剤 / ヒストン脱アセチル化酵素阻害薬
Research Abstract

Chromatin remodeling, caused by histone modifications, plays a crucial role in the regulation of epigenetic gene expression. Histone deacetylase(HDAC) and histone demethylase(HDME) were selected as target enzymes. Isozyme selective and highly active inhibitors against these enzymes were designed and synthesized. HDAC8, SIRT and HDAC3 selective and JMJD2, PHF8, LSD1 selective inhibitors were developed.

  • Research Products

    (24 results)

All 2012 2011 2010 2009 Other

All Journal Article (6 results) Presentation (8 results) Remarks (3 results) Patent(Industrial Property Rights) (7 results)

  • [Journal Article] Lysine demethylases inhibitors2011

    • Author(s)
      Takayoshi Suzuki, Naoki Miyata
    • Journal Title

      J. Med. Chem.

      Volume: 54 Pages: 8236-8250

  • [Journal Article] Design, Synthesis, Enzyme-inhibitory Activity, and Effect on Human Cancer Cells of a Novel Series of Jumonji Domain-Containing Protein 2 Histone Demethylase Inhibitors2010

    • Author(s)
      Shohei Hamada, Takayoshi Suzuki, Koshiki Mino, Koichi Koseki, Felix Oehme, Ingo Flamme, Hiroki Ozasa, Yukihiro Itoh, Daisuke Ogasawara, Haruka Komaarashi, Aiko Katoh, Hiroki Tsumoto, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki
    • Journal Title

      J. Med. Chem.

      Volume: 53 Pages: 5629-5638

  • [Journal Article] An Unexpected Example of Copper-Mediated In Situ Click Chemistry2010

    • Author(s)
      Takayoshi Suzuki, Yosuke Ota, Yuki Kasuya, Motoh Mutsuga, Yoko Kawamura, Hiroki Tsumoto, Hidehiko Nakagawa, M. G. Finn, Naoki Miyata
    • Journal Title

      Angew. Chem. Int. Ed. Engl.

      Volume: 49 Pages: 6817-6820

  • [Journal Article] Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors2009

    • Author(s)
      Rie Ueda, Takayoshi Suzuki, Koshiki Mino, Hiroki Tsumoto, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata
    • Journal Title

      J. Am. Chem. Soc.

      Volume: 131 Pages: 17536-17537

  • [Journal Article] Inhibition of Human Sirtuins by In Situ Generation of an Acetylated Lysine-ADP-ribose Conjugate2009

    • Author(s)
      Tomomi Asaba, Takayoshi Suzuki, Rie Ueda, Hiroki Tsumoto, Hidehiko Nakagawa, Naoki Miyata
    • Journal Title

      J. Am. Chem. Soc.

      Volume: 31 Pages: 6989-6996

  • [Journal Article] Design, Synthesis, and Biological Activity of Boronic acid-Based Histone Deacetylase Inhibitors2009

    • Author(s)
      Nobuaki Suzuki, Takayoshi Suzuki, Yosuke Ota, Tatsuya Nakano, Masaaki Kurihara, Haruhiro Okuda, Takao Yamori, Hiroki Tsumoto, Hidehiko Nakagawa, Naoki Miyata
    • Journal Title

      J. Med. Chem.

      Volume: 52 Pages: 2909-2922

  • [Presentation] Discovery of isozyme-selective histone deacetylase inhibitors by click chemistry2012

    • Author(s)
      Takayoshi Suzuki, Hidehiko Nakagawa, Naoki Miyata, et. al.
    • Organizer
      ACS National Meetng, Sprong 2012
    • Place of Presentation
      San Diego
    • Year and Date
      2012-03-25
  • [Presentation] Design, Synthesis, and Biological Activity of cyclopropylamine-based LSD1 inhibitor2011

    • Author(s)
      Daisuke Ogasawara, Takayoshi Suzuki, Hidehiko Nakagawa, Naoki Miyata, et. al.
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      東京
    • Year and Date
      20111129-1202
  • [Presentation] 創薬化学のすすめ:タンパク質の翻訳後修飾を阻害する化合物の創生を例にして2011

    • Author(s)
      宮田直樹
    • Organizer
      創薬懇話会2011
    • Place of Presentation
      岡山
    • Year and Date
      20110706-07
  • [Presentation] Discovery of selective inhibitors of lysine specific demethylase-12010

    • Author(s)
      T. Suzuki, H. Nakagawa, N. Miyata, et. al.
    • Organizer
      Pacifichem 2010
    • Place of Presentation
      Honolulu, USA
    • Year and Date
      20101215-20
  • [Presentation] Identification of isozyme-selective histone deacetylase inhibitors by click chemistry2010

    • Author(s)
      Y. Kasuya, N. Miyata, et. al.
    • Organizer
      Pacifichem2010
    • Place of Presentation
      Honolulu, USA
    • Year and Date
      20101215-20
  • [Presentation] エピジェネティックに遺伝子発現を制御する低分子化合物の設計と合成2010

    • Author(s)
      宮田直樹
    • Organizer
      第38回構造活性相関シンポジウム
    • Place of Presentation
      徳島
    • Year and Date
      2010-10-31
  • [Presentation] エエピジェネティックに遺伝子発現を制御する化合物:新たな制がん剤の開発をめざして2009

    • Author(s)
      宮田直樹
    • Organizer
      第2回Cancer Research Seminar
    • Place of Presentation
      愛知
    • Year and Date
      2009-11-18
  • [Presentation] HDAC6非感受性阻害薬の創製とその多発性骨髄腫細胞増殖抑制機構の解明2009

    • Author(s)
      宮田直樹、他
    • Organizer
      日本ケミカルバイオロジー学会第4回年会
    • Place of Presentation
      兵庫
    • Year and Date
      2009-05-19
  • [Remarks] 新聞/WEB報道朝日新聞、読売新聞、平成24年2月16日。共同通信、平成24年2月16日。

    • URL

      http://www.47news.jp/CN/201202/CN2012021601001686.html

  • [Remarks] 専門学術紹介記事SciBX, 46, p. 3,(2009).

  • [Remarks]

    • URL

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

  • [Patent(Industrial Property Rights)] 新規ヒドロキサム酸誘導体及びその用途2012

    • Inventor(s)
      宮田直樹、他
    • Industrial Property Rights Holder
      名古屋市立大学、他
    • Industrial Property Number
      特許、2012-38977
    • Filing Date
      2012-02-24
  • [Patent(Industrial Property Rights)] 新規アミド化合物及びその用途2012

    • Inventor(s)
      宮田直樹、他
    • Industrial Property Rights Holder
      名古屋市立大学
    • Industrial Property Number
      特許、2012-37082
    • Filing Date
      2012-02-23
  • [Patent(Industrial Property Rights)] 抗うつ薬及びその用途2010

    • Inventor(s)
      宮田直樹、他
    • Industrial Property Rights Holder
      名古屋市立大学、他
    • Industrial Property Number
      特許、2010-196993
    • Filing Date
      2010-09-02
  • [Patent(Industrial Property Rights)] HIV複製阻害剤2010

    • Inventor(s)
      宮田直樹、他
    • Industrial Property Rights Holder
      名古屋市立大学、他
    • Industrial Property Number
      特許、2010-477176
    • Filing Date
      2010-08-06
  • [Patent(Industrial Property Rights)] ヒドロキサム酸誘導体及びそれを用いたHDAC8阻害剤2010

    • Inventor(s)
      宮田直樹、他
    • Industrial Property Rights Holder
      名古屋市立大学、他
    • Industrial Property Number
      特許、2010-011431
    • Filing Date
      2010-01-21
  • [Patent(Industrial Property Rights)] ヒドロキサム酸誘導体及びJHDM阻害剤2010

    • Inventor(s)
      宮田直樹、他
    • Industrial Property Rights Holder
      名古屋市立大学、他
    • Industrial Property Number
      特許、2010-009834
    • Filing Date
      2010-01-20
  • [Patent(Industrial Property Rights)] LSD阻害剤2009

    • Inventor(s)
      宮田直樹、他
    • Industrial Property Rights Holder
      名古屋市立大学、他
    • Industrial Property Number
      特許、2009-140553
    • Filing Date
      2009-06-11

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Published: 2013-07-31  

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