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Chemical approach towards identifying a putative receptor of N-phosphorylated proteins

Research Project

Project/Area Number 17K08382
Research Category

Grant-in-Aid for Scientific Research (C)

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

Principal Investigator

Yamaguchi Yasuchika  長崎国際大学, 薬学部, 教授 (10183980)

Project Period (FY) 2017-04-01 – 2021-03-31
Project Status Completed (Fiscal Year 2020)
Budget Amount *help
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2020: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2019: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2018: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2017: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
KeywordsN-リン酸化 / ホスホヒスチジン / ペプチドライブラリー / ケミカルバイオロジー / 情報伝達系 / 有機合成化学
Outline of Final Research Achievements

The original aim of this project was to develop a new methodology for finding unknown receptor proteins that recognize N-phosphorylated proteins. We used chemically stable N-phosphorylated amino acid analogs and peptides for our purpose. Thus, we tried to find out a new information system that uses N-phosphorylation as an intermediate.
So far what we have achieved are following: We have synthesized several stable phopho-amino acid analogs, which could be incorporated into peptide libraries. Within our library we discovered exceptionally active lead compounds for an infectious disease project. Since the medical need of this field is huge, we continue medicinal chemistry efforts with these findings.

Academic Significance and Societal Importance of the Research Achievements

当初の目的は、N-リン酸化タンパク質の受容体タンパク質を見つけ出す方法論の開発という基礎的なものであった。研究の過程で多くの新規化合物を合成した。これらを感染症プロジェクトの評価系にかけたところ、これまでの知見では説明できない活性化合物を発見できた。つまり新しいメカニズムをもつ医薬品創成に役立つ結果である。感染症分野の新薬の期待は大きいことから、この発見を実際の創薬につなげていく予定である。

Report

(5 results)
  • 2020 Annual Research Report   Final Research Report ( PDF )
  • 2019 Research-status Report
  • 2018 Research-status Report
  • 2017 Research-status Report
  • Research Products

    (8 results)

All 2021 2019 2018 2017

All Journal Article (2 results) (of which Int'l Joint Research: 1 results,  Peer Reviewed: 2 results) Presentation (2 results) (of which Invited: 1 results) Book (4 results)

  • [Journal Article] Selective and reversible modification of kinase cysteines with chlorofluoroacetamides2019

    • Author(s)
      Shindo N, Fuchida H,Sato Mi, Watari K, Shibata T, Kuwata K, Miura C, Okamoto K, Hatsuyama Y, Tokunaga K, Sakamoto S, Morimoto S, Abe Y, Shiroishi M, Caaveiro J. M. M., Ueda T, Tamura T, Matsunaga N, Nakao T, Koyanagi S, Ohdo S, Yamaguchi Y, Hamachi I, Ono M, Ojida A
    • Journal Title

      Nature Chemical Biology

      Volume: 15 Issue: 3 Pages: 250-258

    • DOI

      10.1038/s41589-018-0204-3

    • Related Report
      2018 Research-status Report
    • Peer Reviewed
  • [Journal Article] Establishment of a quantitative and qualitative analysis and isolation method for tetracyclic iridoids from Morinda lucida Bentham leaves.2019

    • Author(s)
      Ohta T, Tilkanont T, Ayertey F, Nakagawa M, Tung NH, Bolah P, Blagogee H, Appiah AA, Ocloo A, Ohashi M, Tanoue K, Yamaguchi Y, Ohta N, Yamaoka S, Iwanaga S, Uto T, Shoyama S.
    • Journal Title

      Journal of Pharmaceutical and Biomedical Analysis

      Volume: 164 Pages: 475-480

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Int'l Joint Research
  • [Presentation] Morinda lucida含有テトラサイクリックイリドイドの定量分析法の開発2018

    • Author(s)
      太田智絵,Tanatorn Tilkanont,Nguyen Huu Tung, Frederick Ayertey,田上兼輔,Alfred A. Appiah,Augustine Ocloo,大橋光子,宇都拓洋,山口泰史,岩永史郎,太田伸生,正山征洋
    • Organizer
      日本薬学会第138年会(金沢)
    • Related Report
      2018 Research-status Report
  • [Presentation] いかにして、活性ある化合物(functionally active compounds)を見つけだすか?:先人に学ぶ2017

    • Author(s)
      山口 泰史
    • Organizer
      日産化学株式会社 創薬セミナー
    • Related Report
      2017 Research-status Report
    • Invited
  • [Book] 現場で役に立つ! 臨床医薬品化学2021

    • Author(s)
      臨床医薬品化学研究会
    • Total Pages
      264
    • Publisher
      化学同人
    • ISBN
      9784759820546
    • Related Report
      2020 Annual Research Report
  • [Book] 薬系 有機化学2018

    • Author(s)
      安藤 章、山口 泰史 他
    • Total Pages
      454
    • Publisher
      南江堂
    • ISBN
      9784524403349
    • Related Report
      2017 Research-status Report
  • [Book] 新編 医薬化学2018

    • Author(s)
      日比野、石倉、北川、須本、波多江、山口 泰史 他
    • Total Pages
      368
    • Publisher
      廣川書店
    • ISBN
      9784567461566
    • Related Report
      2017 Research-status Report
  • [Book] 大学生のための有機反応問題集 第2版2018

    • Author(s)
      山口 泰史
    • Total Pages
      120
    • Publisher
      三共出版
    • ISBN
      9784782707777
    • Related Report
      2017 Research-status Report

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Published: 2017-04-28   Modified: 2022-01-27  

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