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Drug discovery research for clinical application of PCA-1 inhibitors

Research Project

Project/Area Number 15K08036
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionHyogo University of Health Sciences

Principal Investigator

TOKORO(MABUCHI) Miyuki  兵庫医療大学, 薬学部, 研究員 (60714897)

Co-Investigator(Kenkyū-buntansha) 辻川 和丈  大阪大学, 薬学研究科, 教授 (10207376)
田中 明人  兵庫医療大学, 薬学部, 教授 (30454789)
Project Period (FY) 2015-04-01 – 2018-03-31
Project Status Completed (Fiscal Year 2017)
Budget Amount *help
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2016: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2015: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
KeywordsPCA-1 / ALKBH3 / 抗がん剤 / 前立腺がん / Docetaxel / 併用効果 / 悪性中皮腫 / MESO-4 / PCA-1 / ALKBH3 / 前立腺癌 / 中皮腫 / Cisplatin / 前立腺
Outline of Final Research Achievements

We previously developed a novel PCA-1 inhibitor, named HUHS015. We examine anti-cancer effects of HUHS015 in combination with known anti-cancer drugs in our continuous studies. In this study, hormone-independent prostate cancers and malignant mesothelioma were used. We found synagistic effects of HUHS015 in vitro in combination with Docetaxel and Cisplatin, which were often clinically used for hormone-independent prostate cancers treatment. We also found that combinational treatment of HUHS015 with Cisplatin, Irinotecan, Doxorubicin, Vinorelbine and Gemcitabine in malignant mesothelioma synergistically inhibited growth of malignant mesothelioma cells in vitro. Furthermore, additive effects of HUHS015 comibinatorial uses with Docetaxel in vivo were demonstrated, that is, administration of 1 and 2.5 mg/kg of Docetaxel with 32 mg/kg of HUHS015 were more potent than that of only Docetaxel administrations.

Report

(4 results)
  • 2017 Annual Research Report   Final Research Report ( PDF )
  • 2016 Research-status Report
  • 2015 Research-status Report
  • Research Products

    (5 results)

All 2018 2017 2016 2015

All Journal Article (4 results) (of which Peer Reviewed: 4 results,  Acknowledgement Compliant: 1 results) Presentation (1 results)

  • [Journal Article] Novel Metabolically Stable PCA-1/ALKBH3 Inhibitor Has Potent Antiproliferative Effects on DU145 Cells In Vivo.2018

    • Author(s)
      Ueda M, Shimizu T, Mabuchi M, Horiike K, Kitae K, Hase H, Ueda Y, Tsujikawa K, Tanaka A
    • Journal Title

      Anticancer Res.

      Volume: 38 Issue: 1 Pages: 211-218

    • DOI

      10.21873/anticanres.12210

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Systematic Trial for Evaluating Docetaxel in a Human Prostate Cancer Cell DU145 Xenograft Model2017

    • Author(s)
      MIYUKI MABUCHI, MASAHIRO UEDA, YURI YOSHIDA, KOTA HORIIKE, KENTA YAMAOKA, SYUHEI NAKAO, TADASHI SHIMIZU, YUKO UEDA, KAZUTAKE TSUJIKAWA, AKITO TANAKA
    • Journal Title

      anticancer research

      Volume: 37 Issue: 4 Pages: 1665-1676

    • DOI

      10.21873/anticanres.11496

    • Related Report
      2016 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Identification and purification of target protein using affinity resin bearing a photo-labile linker.2015

    • Author(s)
      Mabuchi M,Shimizu T,Haramura M,Tanaka A
    • Journal Title

      Bioorg Med Chem Lett.

      Volume: 25 Issue: 16 Pages: 3373-3377

    • DOI

      10.1016/j.bmcl.2015.05.023

    • Related Report
      2015 Research-status Report
    • Peer Reviewed
  • [Journal Article] 3.Improvement of solid material for affinity resins by application of long PEG spacers to capture the whole target complex of FK5062015

    • Author(s)
      Mabuchi M, Shimizu T, Ueda M, Mitamura K, Ikegawa S, Tanaka A.
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 25 Issue: 14 Pages: 2788-2792

    • DOI

      10.1016/j.bmcl.2015.05.014

    • Related Report
      2015 Research-status Report
    • Peer Reviewed
  • [Presentation] 新規固相担体AquaFirmusの応用研究(1)2016

    • Author(s)
      馬渕美雪
    • Organizer
      日本ケミカルバイオロジー学会第11回年会
    • Place of Presentation
      京都テルサ テルサホール(京都府京都市)
    • Year and Date
      2016-06-15
    • Related Report
      2015 Research-status Report

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Published: 2015-04-16   Modified: 2019-03-29  

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