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Elucidation of androgen-dependent growth inhibition mechanism in prostate cancer of novel small molecule compound APA

Research Project

Project/Area Number 15K10615
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Urology
Research InstitutionMicrobial Chemistry Research Foundation

Principal Investigator

YAMAZAKI Yohko  公益財団法人微生物化学研究会, 微生物化学研究所 沼津支所, 研究員 (80342690)

Co-Investigator(Renkei-kenkyūsha) MOMOSE Isao  公益財団法人微生物化学研究会, 微生物化学研究所沼津支所, 主席研究員 (10270547)
ABE Hikaru  公益財団法人微生物化学研究会, 微生物化学研究所, 研究員 (10462269)
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: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Keywords前立腺がん / アンドロゲンレセプター
Outline of Final Research Achievements

Although endocrine therapy is the mainstay of treatment for advanced prostate cancer, most patients with prostate cancer progress from androgen-dependent to castration-resistant (CRPC) disease. Androgen receptor (AR) is required for CRPC progression, but AR inhibitors are antagonists only.
We discovered androprostamine (APA) , a novel inhibitor of androgen-dependent human prostate cancer cell growth, from microbial metabolite. APA showed better antitumor activity than clinically used bicalutamide in in vivo experiments using mice, but side effects such as weight loss were observed. Therefore, we synthesized 50 kinds of derivatives based on APA and succeeded in synthesis of new derivatives which keep antitumor activity with reduced side effects.

Report

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

    (8 results)

All 2017 2016 2015 Other

All Journal Article (2 results) (of which Int'l Joint Research: 1 results,  Peer Reviewed: 2 results,  Open Access: 2 results) Presentation (5 results) (of which Int'l Joint Research: 2 results,  Invited: 1 results) Remarks (1 results)

  • [Journal Article] Synthesis of Androprostamine A and Resormycin2016

    • Author(s)
      H. Abe, Y. Yamazaki, C. Sakashita, I. Momose, T. Watanabe, M. Shibasaki
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 64 Issue: 7 Pages: 982-987

    • DOI

      10.1248/cpb.c16-00207

    • NAID

      130005160028

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2016 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Biological activities of unique isoflavones prepared from Apios americana Medik.2016

    • Author(s)
      Kaneta H, Koda M, Saito S, Imoto M, Kawada M, Yamazaki Y, Momose I, Shindo K.
    • Journal Title

      Biosci Biotechnol Biochem

      Volume: 80 Issue: 4 Pages: 774-778

    • DOI

      10.1080/09168451.2015.1127132

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Presentation] AS1936: A new inhibitor of androgen receptor function in prostate cancer2017

    • Author(s)
      Yohko Yamazaki, Shun-ichi Ohba, Hikaru Abe, Takumi Watanabe, Isao Momose, Manabu Kawada, Masakatsu Shibasaki
    • Organizer
      第76回日本癌学会学術総会
    • Related Report
      2017 Annual Research Report
  • [Presentation] Androprostamine A, a New Antitumor Agent for Castration Resistant Prostate Cancer2016

    • Author(s)
      Yohko YAMAZAKI, Tohru MASUDA, Isao MOMOSE, Manabu KAWADA, Akio NOMOTO, Masakatsu SHIBASAKI
    • Organizer
      2nd International Symposium for Medicinal Sciences
    • Place of Presentation
      パシフィコ横浜(横浜)
    • Year and Date
      2016-03-28
    • Related Report
      2015 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] Construction of screening system for new AR signaling inhibitors2016

    • Author(s)
      Yohko Yamazaki, Isao Momose, Manabu Kawada, Masakatsu Shibasaki
    • Organizer
      第10回日米癌合同会議
    • Place of Presentation
      Hyatt Regency Maui/Maui
    • Year and Date
      2016-02-19
    • Related Report
      2015 Research-status Report
    • Int'l Joint Research
  • [Presentation] Construction of screening system for a novel AR signaling inhibitor2015

    • Author(s)
      Yohko Yamazaki, Isao momose, Manabu Kawada, Masakatsu Shibasaki
    • Organizer
      第74回日本癌学会学術総会
    • Place of Presentation
      名古屋国際会議場/名古屋
    • Year and Date
      2015-10-09
    • Related Report
      2015 Research-status Report
  • [Presentation] 新規抗前立腺がん物質androprostamine Aの抗腫瘍活性2015

    • Author(s)
      山崎洋子 増田徹 川田学 百瀬功 柴﨑正勝
    • Organizer
      第19回日本がん分子標的治療学会
    • Place of Presentation
      松山全日空ホテル/松山
    • Year and Date
      2015-06-12
    • Related Report
      2015 Research-status Report
  • [Remarks] IMC 微生物化学研究所

    • URL

      http://www.bikaken.or.jp

    • Related Report
      2016 Research-status Report 2015 Research-status Report

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

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