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Molecular mechanism of the tissue-specific expression of the hydrolases which enzymes related to structure activity relationship of pro-drugs

Research Project

Project/Area Number 24590206
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Medical pharmacy
Research InstitutionChiba Institute of Science

Principal Investigator

HOSOKAWA Masakiyo  千葉科学大学, 薬学部, 教授 (70181500)

Project Period (FY) 2012-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2013: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2012: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Keywordsカルボキシルエステラーゼ / プロドラッグ / 代謝活性化 / AADAC / 薬物代謝酵素 / パラオクソナーゼ / ブチリルコリンエステラーゼ / アリルアセトアミドデアセチラーゼ / CES / PON / エステラーゼ
Outline of Final Research Achievements

Human carboxylesterase (CES), butyrylcholinesterase (BuChE), arylacetamido deacetylase (AADAC), cholesteroesterase(ChlE) and paraoxonase (PON) efficiently catalyze the hydrolysis of a variety of ester- and amide-containing chemicals as well as drug to the respective free acid. These hydrolases catalyze the hydrolysis of the different structure of clinically used pro-drugs. In this study, we investigated the tissue specific expression and the structure activity relationship of pro-drugs of these hydrolase enzymes.

Report

(4 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Research-status Report
  • 2012 Research-status Report
  • Research Products

    (13 results)

All 2015 2014 2013 2012

All Journal Article (5 results) (of which Peer Reviewed: 5 results,  Open Access: 1 results) Presentation (3 results) Book (5 results)

  • [Journal Article] Isolation and characterization of arylacetamide deacetylase in cynomolgus macaques2015

    • Author(s)
      Uno Y, Hosokawa M, Imai T
    • Journal Title

      J Vet Med Sci

      Volume: 印刷中

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Systematic identification andcharacterization of carboxylesterases in cynomolgus macaques.2014

    • Author(s)
      Uno Y Uehara S, Hosokawa M, Imai T
    • Journal Title

      Drug Metab Dispos.

      Volume: 42 Issue: 12 Pages: 2002-2006

    • DOI

      10.1124/dmd.114.059972

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] The effect of carboxylesterase 1 (CES1) polymorphisms on the pharmacokinetics of oseltamivir in humans.2013

    • Author(s)
      Suzaki Yuki
    • Journal Title

      Eur J Clin Pharmacol.

      Volume: 69(1) Issue: 1 Pages: 21-30

    • DOI

      10.1007/s00228-012-1315-5

    • Related Report
      2013 Research-status Report 2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Gly143Glu polymorphism of the human carboxylesterase1 gene in an Asian population.2013

    • Author(s)
      Suzaki Yuki
    • Journal Title

      Eur J Clin Pharmacol.

      Volume: 69(3) Issue: 3 Pages: 735-736

    • DOI

      10.1007/s00228-012-1352-0

    • Related Report
      2013 Research-status Report 2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Dexamethasone-mediated transcriptional regulation of rat carboxylesterase 2 gene2012

    • Author(s)
      Hori T, Jin L, Fujii A, Furihata T, Nagahara Y, Chiba K, Hosokawa M.
    • Journal Title

      Xenobiotica

      Volume: 42 Issue: 7 Pages: 614-623

    • DOI

      10.3109/00498254.2011.648670

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Presentation] Dexamethasone mediate transcriptional regulation of carboxylesterase 1A1 gene in human fetal liver cells2014

    • Author(s)
      Hosokawa Masakiyo, Hori Takeshi. Matsuanga Tamihide, Ohmori Shigeru
    • Organizer
      19th North American ISSX Meeting and 29th JSSX Annual Meeting,
    • Place of Presentation
      San Francisco, California, USA,
    • Year and Date
      2014-10-18 – 2014-10-23
    • Related Report
      2014 Annual Research Report
  • [Presentation] Enzymatic characteristics of monkey and human carboxyl esterase 2 and its age-dependent expression2012

    • Author(s)
      Ohura K, Fujihara S, Uno Y, Hosokawa M, Imai T
    • Organizer
      日本薬物動態学会
    • Place of Presentation
      東京
    • Related Report
      2012 Research-status Report
  • [Presentation] Characterization and properties of cynomolgus monkey carboxyl esterase (CES) isozymes2012

    • Author(s)
      Ishida T, Sudou A, Hatano Y, Uno Y, Imai T, Hosokawa M
    • Organizer
      日本薬物動態学会
    • Place of Presentation
      東京
    • Related Report
      2012 Research-status Report
  • [Book] 酵素誘導実験 薬剤学実験法必携マニュアルII生物薬剤学(日本薬剤学会編集委員会編)2014

    • Author(s)
      細川正清
    • Publisher
      南江堂
    • Related Report
      2014 Annual Research Report
  • [Book] 9章1-5異物代謝に影響を及ぼす因子 衛生薬学-健康と環境-(永沼章、姫野誠一郎、平塚明編)2014

    • Author(s)
      細川正清
    • Publisher
      丸善出版
    • Related Report
      2014 Annual Research Report
  • [Book] 薬剤学実験法必携マニュアルII生物薬剤学 第5章薬物代謝実験2014

    • Author(s)
      細川正清 他56名
    • Total Pages
      423
    • Publisher
      南江堂
    • Related Report
      2013 Research-status Report
  • [Book] 衛生薬学 第9章化学物質と毒性2013

    • Author(s)
      細川正清 他25名
    • Total Pages
      503
    • Publisher
      丸善出版
    • Related Report
      2013 Research-status Report
  • [Book] 衛生薬学  第9章 化学物質と毒性2013

    • Author(s)
      細川正清 他22名
    • Total Pages
      503
    • Publisher
      丸善出版
    • Related Report
      2012 Research-status Report

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Published: 2013-05-31   Modified: 2019-07-29  

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