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Development of SIRT6 activators targeting for Warburg effect

Research Project

Project/Area Number 15K18899
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionNagoya City University

Principal Investigator

Kawaguchi Mitsuyasu  名古屋市立大学, 大学院薬学研究科, 助教 (10735682)

Project Period (FY) 2015-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2016: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2015: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
KeywordsSirtuin / 蛍光プローブ / ワールブルグ効果
Outline of Final Research Achievements

In general, sirtuin activity is detectable by a protease (eg. trypsin) coupled two-steps method. However, such method has several problems, cumbersome procedure, false-positive compounds on chemical screening.
In this study, focusing on interesting reports showing that sirtuin recognize and hydrolize long-chain fatty acyl groups, we hypothesized that sirtuin can hydrolize acyl groups of large quencher dyes. We exhibited that sirtuin activity is detectable by a FRET based novel fluorescence probe, SFP3, and applied this methodology for chemical screening. We identified novel scaffolds of SIRT6 inhibitor and activiator.

Report

(3 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • Research Products

    (18 results)

All 2017 2016 2015

All Journal Article (7 results) (of which Int'l Joint Research: 1 results,  Peer Reviewed: 7 results,  Open Access: 6 results,  Acknowledgement Compliant: 3 results) Presentation (11 results) (of which Int'l Joint Research: 2 results)

  • [Journal Article] A yellowish-green-light-controllable nitric oxide donor based on N-nitrosoaminophenol applicable for photocontrolled vasolidation2017

    • Author(s)
      Okuno H, Ieda N, Hotta Y, Kawaguchi M, Kimura K, Nakagawa H.
    • Journal Title

      Org. Biomol. Chem.

      Volume: 15 Issue: 13 Pages: 2791-2796

    • DOI

      10.1039/c7ob00245a

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] Visible Light-Controlled Nitric Oxide Release from Hindered Nitrobenzene Derivatives for Specific Modulation of Mitochondrial Dynamics2016

    • Author(s)
      Kai Kitamura, Mitsuyasu Kawaguchi, Naoya Ieda, Naoki Miyata, and Hidehiko Nakagawa
    • Journal Title

      ACS Chem. Biol.

      Volume: 11 Issue: 5 Pages: 1271-1278

    • DOI

      10.1021/acschembio.5b00962

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] (7-Diethylaminocomarin-4-yl)methyl Ester of Suberoylanilide Hydroxamic Acid as a Caged Inhibitor for Photocontrol of Histone Deacetylase Activity2016

    • Author(s)
      Naoya Ieda, Sota Yamada, Mitsuyasu Kawaguchi, Naoki Miyata, and Hidehiko Nakagawa
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 24 Issue: 12 Pages: 2789-2793

    • DOI

      10.1016/j.bmc.2016.04.042

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Fluorescence Probe for Imaging Sirtuin Activity in Living Cells, Based on One-Step Cleavage of Dabcyl Quencher2016

    • Author(s)
      Kawaguchi M, Ikegawa S, Ieda N, Nakagawa H.
    • Journal Title

      ChemBioChem

      Volume: 17 Issue: 20 Pages: 1961-1967

    • DOI

      10.1002/cbic.201600374

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] A double bond-conjugated dimethylnitrobenzene-type photolabile nitric oxide donor with improved two-photon cross section2015

    • Author(s)
      1.N. Ieda, K. Hishikawa, K. Eto, K. Kitamura, M. Kawaguchi, T. Suzuki, K. Fukuhara, N. Miyata, T. Furuta, J. Nabekura, H. Nakagawa
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 25 Issue: 16 Pages: 3172-3175

    • DOI

      10.1016/j.bmcl.2015.05.095

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Identification of tissue-restricted bio-reaction suitable for in vivo targeting by fluorescent substrate library-based enzyme discovery2015

    • Author(s)
      Kentaro Yoshioka, Toru Komatsu, Akihiro Nakada, Jun Onagi, Yugo Kuriki, Mitsuyasu Kawaguchi, Takuya Terai, Tasuku Ueno, Kenjiro Hanaoka, Tetsuo Nagano, and Yasuteru Urano
    • Journal Title

      J. Am. Chem. Soc.

      Volume: 137 Issue: 38 Pages: 12187-12190

    • DOI

      10.1021/jacs.5b05884

    • Related Report
      2015 Research-status Report
    • Peer Reviewed
  • [Journal Article] Peptidyl prolyl isomerase Pin1-inhibitory activity of D-glutamic and D-aspartic acid derivatives bearing a cyclic aliphatic amine moiety2015

    • Author(s)
      Nakagawa H, Seike S, Sugimoto M, Ieda N, Kawaguchi M, Suzuki T, Miyata N.
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 25 Issue: 23 Pages: 5619-5624

    • DOI

      10.1016/j.bmcl.2015.10.033

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Open Access
  • [Presentation] SIRT6活性検出蛍光プローブの開発とケミカルスクリーニング2017

    • Author(s)
      川口充康、池川祥平、家田直弥、中川秀彦
    • Organizer
      日本薬学会第137年会
    • Place of Presentation
      仙台
    • Year and Date
      2017-03-24
    • Related Report
      2016 Annual Research Report
  • [Presentation] Sirtuin蛍光プローブの開発と生細胞イメージング2017

    • Author(s)
      川口充康、池川祥平、家田直弥、中川秀彦
    • Organizer
      日本酸化ストレス学会東海支部 第5回学術集会,
    • Place of Presentation
      名古屋
    • Year and Date
      2017-02-18
    • Related Report
      2016 Annual Research Report
  • [Presentation] Sirtuin蛍光プローブの開発と生細胞イメージングへの応用2016

    • Author(s)
      川口充康, 池川祥平、家田直弥, 中川秀彦
    • Organizer
      第14回 がんとハイポキシア研究会
    • Place of Presentation
      岐阜
    • Year and Date
      2016-11-04
    • Related Report
      2016 Annual Research Report
  • [Presentation] SIRT6活性検出プローブの開発とmodulatorの探索2016

    • Author(s)
      池川祥平, 川口充康, 家田直弥, 中川秀彦
    • Organizer
      日本薬学会東海支部 合同学術大会2016
    • Place of Presentation
      岐阜
    • Year and Date
      2016-10-30
    • Related Report
      2016 Annual Research Report
  • [Presentation] Development of one-step sirtuin activity fluorescence probe and living cell imaging2016

    • Author(s)
      Mitsuyasu Kawaguchi, Shohei Ikegawa, Naoya Ieda, Hidehiko Nakagawa
    • Organizer
      ACS National Meeting
    • Place of Presentation
      Philadelphia
    • Year and Date
      2016-08-21
    • Related Report
      2016 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Sirtuin活性検出蛍光プローブの開発と生細胞応用2016

    • Author(s)
      川口充康, 池川祥平, 家田直弥, 中川秀彦
    • Organizer
      日本ケミカルバイオロジー学会第11回年会
    • Place of Presentation
      京都
    • Year and Date
      2016-06-15
    • Related Report
      2016 Annual Research Report
  • [Presentation] Sirtuin活性検出蛍光プローブの開発と生細胞応用2016

    • Author(s)
      川口充康、池川祥平、家田直弥、中川秀彦
    • Organizer
      ケミカルバイオロジー学会第11回年会
    • Place of Presentation
      京都
    • Year and Date
      2016-06-15
    • Related Report
      2015 Research-status Report
  • [Presentation] Sirtuin活性検出蛍光プローブの開発と細胞イメージング2016

    • Author(s)
      川口充康, 池川祥平, 家田直弥, 中川秀彦
    • Organizer
      第14回次世代を担う有機化学シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2016-05-27
    • Related Report
      2016 Annual Research Report
  • [Presentation] Sirtuin活性検出蛍光プローブの開発と細胞イメージング2016

    • Author(s)
      川口充康、池川祥平、家田直弥、中川秀彦
    • Organizer
      第14回次世代シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2016-05-27
    • Related Report
      2015 Research-status Report
  • [Presentation] MITOCHONDRIA-TARGETING NITRIC OXIDE RELEASERS CONTROLLABLE WITH VISIBLE LIGHT AND MODULATION OF MITOCHONDRIAL DYNAMICS2016

    • Author(s)
      Kai Kitamura, Mitsuyasu Kawaguchi, Naoya Ieda, Kazuhiro Hishikawa, Takayoshi Suzuki, Naoki Miyata, Hidehiko Nakagawa
    • Organizer
      26th IUPAC International symposium on photochemistry
    • Place of Presentation
      Osaka
    • Year and Date
      2016-04-03
    • Related Report
      2015 Research-status Report
    • Int'l Joint Research
  • [Presentation] 簡便かつ高感度なSirtuin活性蛍光検出系の構築2016

    • Author(s)
      川口充康、池川祥平、家田直弥、中川秀彦
    • Organizer
      日本薬学会
    • Place of Presentation
      横浜
    • Year and Date
      2016-03-26
    • Related Report
      2015 Research-status Report

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Published: 2015-04-16   Modified: 2018-03-22  

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