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Drug discovery based on a new biological assay system using Yeast knock-out strain collection

Research Project

Project/Area Number 21580130
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Bioproduction chemistry/Bioorganic chemistry
Research InstitutionTokyo Denki University

Principal Investigator

KAWAI Satoru  東京電機大学, 理工学部, 教授 (10328528)

Project Period (FY) 2009 – 2011
Project Status Completed (Fiscal Year 2011)
Budget Amount *help
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2011: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2010: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2009: ¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Keywords出芽酵母 / フラボノイド / クマリン / 合成化学 / 多剤耐性化関連遺伝子 / ABCトランスポーター / Saccharomyces cerevisiae / pdr遺伝子破壊 / フラボノイド類 / クマリン類 / MTT法
Research Abstract

Multidrug resistance(MDR) mediated by broad specificity transporters is one of the most important strategies used by pathogens, including cancer cells, to evade chemotherapy. In the yeast Saccharomyces cerevisiae, a complex pleiotropic drug resistance(PDR) network of genes involved in MDR is composed of the transcriptional regulators which activate expression of the ABC transporters-encoding genes. We have synthesized 154 flavonoids and screened for their antiproliferative activities toward isogenic S. cerevisiae strains deleted of PDR1, PDR3, PDR8, PDR10, PDR11, PDR16 and fluorinated flavonoids demonstrated the specific antiproliferative activity toward pdr1D strains. Our results may contribute to a better understanding of the mechanism of MDR. They also provide the indication of the physiological function of MDR transporters and suggest new approaches for cancer chemotherapy.

Report

(4 results)
  • 2011 Annual Research Report   Final Research Report ( PDF )
  • 2010 Annual Research Report
  • 2009 Annual Research Report
  • Research Products

    (10 results)

All 2012 2011 2010

All Journal Article (4 results) (of which Peer Reviewed: 2 results) Presentation (6 results)

  • [Journal Article] Relationship between structure and antiproliferative activity of 1-azaflavanones2012

    • Author(s)
      Satoru Kawaii, Kotaro Endo, Tetsuo Tokiwano, Yuko Yoshizawa
    • Journal Title

      Anticancer Research

      Volume: (in press)

    • URL

      http://www.iiar-anticancer.org/

    • Related Report
      2011 Final Research Report
  • [Journal Article] Four New Bisabolane-type Sesquiterpenes from Ligularia lankongensis2012

    • Author(s)
      Hiroshi Hirota, Yurie Horiguchi, Satoru Kawaii, Chiaki Kuroda, Ryo Hanai, Xun Gong
    • Journal Title

      Natural Product Communications

      Volume: 7 Pages: 451-454

    • URL

      http://www.naturalproduct.us/

    • Related Report
      2011 Final Research Report
  • [Journal Article] Four new bisabolane-type sesquiterpenes from Ligularia lankongensis2012

    • Author(s)
      Hirota H, Kawaii S, et al
    • Journal Title

      Nat Prod Commun.

      Volume: 7 Pages: 451-454

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Chemical and Genetic Study of Ligularia duciformis and Related Species in Sichuan and Yunnan Provinces of China2012

    • Author(s)
      Nagano H, Kawaii S, et al
    • Journal Title

      Chemistry and Biodiversity

      Volume: 9 Pages: 789-805

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Presentation] フラボノイド関連化合物の合成とノックアウト酵母に対する影響2012

    • Author(s)
      田島知子, 川井悟, ら
    • Organizer
      日本農芸化学会
    • Place of Presentation
      京都女子大学(京都市)
    • Year and Date
      2012-03-25
    • Related Report
      2011 Annual Research Report
  • [Presentation] フラボノイド関連化合物の合成とノックアウト酵母に対する影響2012

    • Author(s)
      田島知子, 川井悟, 常盤野哲生, 中澤伸重, 吉澤結子
    • Organizer
      日本農芸化学会2012年度大会
    • Place of Presentation
      京都
    • Year and Date
      2012-03-24
    • Related Report
      2011 Final Research Report
  • [Presentation] スチルベノイドの合成と遺伝子破壊出芽酵母に対する影響2012

    • Author(s)
      倉持晴樹, 潮見あずさ, 山本夕貴, 川井悟, 常盤野哲生, 中澤伸重, 吉澤結子
    • Organizer
      日本農芸化学会2012年度大会
    • Place of Presentation
      京都
    • Year and Date
      2012-03-24
    • Related Report
      2011 Final Research Report
  • [Presentation] フラボノイド類縁体の合成とノックアウト酵母増殖抑制効果2011

    • Author(s)
      川井悟
    • Organizer
      日本農芸化学会2011年度大会
    • Place of Presentation
      京都・京都女子大学
    • Year and Date
      2011-03-27
    • Related Report
      2010 Annual Research Report
  • [Presentation] スチルベン類の合成と遺伝子破壊出芽酵母に対する影響2011

    • Author(s)
      川井悟
    • Organizer
      日本農芸化学会2011年度大会
    • Place of Presentation
      京都・京都女子大学
    • Year and Date
      2011-03-27
    • Related Report
      2010 Annual Research Report
  • [Presentation] ノックアウト酵母コレクションを利用した生理活性物質の探索2010

    • Author(s)
      川井悟
    • Organizer
      日本農芸化学会
    • Place of Presentation
      東京大学
    • Year and Date
      2010-03-29
    • Related Report
      2009 Annual Research Report

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Published: 2009-04-01   Modified: 2016-04-21  

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