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Synthesis of PEGylated drug candidates for PET imaging

Research Project

Project/Area Number 24659049
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionOsaka University (2013-2014)
University of Shizuoka (2012)

Principal Investigator

AKAI Shuji  大阪大学, 薬学研究科(研究院), 教授 (60192457)

Co-Investigator(Renkei-kenkyūsha) OKU Naoto  静岡県立大学, 薬学部, 教授 (10167322)
Project Period (FY) 2012-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2013: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2012: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsポリエチレングリコール / クリック化学 / ペプチド / PEG化医薬品 / イメージング / 創薬 / フッ素アニオン / 蛍光色素 / PEG / Huisgen反応 / フッ素化 / 体内動態解析 / PEG化医薬品 / フルオラス化学
Outline of Final Research Achievements

The covalent attachment of poly(ethylene glycol) (PEG) with an average molecular weight (Mw) of 5-40 kDa to a drug or a therapeutic protein, called PEGylation, is a common strategy to evade the host immune system, to enhance its stability in blood, etc. In this study, we have developed a synthetic method of PEGylated peptides, possessing a fluorescent moiety at one end of the PEG chain, which enabled noninvasive whole-body trafficking of such molecules in living rats.

Report

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

    (5 results)

All 2014 2013

All Journal Article (2 results) (of which Peer Reviewed: 2 results,  Open Access: 1 results,  Acknowledgement Compliant: 1 results) Presentation (1 results) Patent(Industrial Property Rights) (2 results) (of which Overseas: 1 results)

  • [Journal Article] Real-time trafficking of PEGylated liposomes in the rodent focal brain ischemia analyzed by positron emission tomography2014

    • Author(s)
      Fukuta T, Ishii T, Asai T, Nakamura G, Takeuchi Y, Sato A, Agato Y, Shimizu K, Asai S, Fukumoto D, Harada N, Tsukada H, Kawaguchi AT, Oku N
    • Journal Title

      Artificial organs

      Volume: 38 Issue: 8 Pages: 662-6

    • DOI

      10.1111/aor.12350

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Dynamic Analysis of Fluid Distribution in the Gastrointestinal Tract in Rats: Positron Emission Tomography Imaging after Oral Administration of Nonabsorbable Marker, [(18)F]Deoxyfluoropoly(ethylene glycol)2013

    • Author(s)
      Takashima T, Shingaki T, Katayama Y, Hayashinaka E, Wada Y, Kataoka M, Ozaki D, Doi H, Suzuki M, Ishida S, Hatanaka K, Sugiyama Y, Akai S, Oku N, Yamashita S, Watanabe Y
    • Journal Title

      Mol. Pharmaceutics

      Volume: 10 Issue: 6 Pages: 2261-2269

    • DOI

      10.1021/mp300469m

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Presentation] 長鎖PEGを結合したがん細胞親和性ペプチドの合成とそ非侵襲的体内動態解析2014

    • Author(s)
      赤井周司、澤田健太郎、他
    • Organizer
      第32回メディシナルケミストリーシンポジウム
    • Place of Presentation
      兵庫県、神戸市
    • Year and Date
      2014-11-26 – 2014-11-28
    • Related Report
      2014 Annual Research Report
  • [Patent(Industrial Property Rights)] [18F]Fまたは蛍光色素で標識されたPEG化生物活性化合物の製造方法、ならびにその体内動態解析2014

    • Inventor(s)
      赤井周司,奥 直人
    • Industrial Property Rights Holder
      赤井周司,奥 直人
    • Industrial Property Rights Type
      特許
    • Filing Date
      2014-03-27
    • Related Report
      2013 Research-status Report
    • Overseas
  • [Patent(Industrial Property Rights)] [18F]Fまたは蛍光色素で標識されたPEG化生物活性化合物の製造方法、ならびにその体内動態解析2013

    • Inventor(s)
      赤井周司,奥 直人
    • Industrial Property Rights Holder
      静岡県立大学
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2013-070277
    • Filing Date
      2013-03-28
    • Related Report
      2012 Research-status Report

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

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