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2012 Fiscal Year Final Research Report

Development of selective phosphatase inhibitor based on calyculin A

Research Project

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Project/Area Number 23710250
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Living organism molecular science
Research InstitutionThe University of Tokyo

Principal Investigator

TOSHIYUKI Wakimoto  東京大学, 大学院・薬学系研究科, 准教授 (70363900)

Project Period (FY) 2011 – 2012
Keywordsカリクリン / タンパク質脱リン酸化酵素 / チョコガタイシカイメン
Research Abstract

Many marine natural products exhibit highly potent cytotoxicity. They selectively inhibit the functions of either intracellular or membrane-bound target molecules, leading to cell death. These specific biological activities can provide valuable information on the biochemical research field. Therefore, we initiated this program aimed at the development of functionalized calyculin A, a protein phosphatase inhibitor, which was originally isolated from the marine sponge, Discodermia calyx. Based on the insights into the structural moieties essential for biological activity, the synthetic process toward library construction and fluorescent probe were developed.

  • Research Products

    (12 results)

All 2013 2012 2011 Other

All Journal Article (6 results) (of which Peer Reviewed: 6 results) Presentation (5 results) Remarks (1 results)

  • [Journal Article] Allos- hemicalyculin A, a photochemically converted calyculin fromthe marine sponge Discodermia calyx2013

    • Author(s)
      M. Kimura, T. Wakimoto, I. Abe
    • Journal Title

      Tetrahedron Lett

      Volume: 54 Pages: 114-116

    • DOI

      DOI:10.1016/j.tetlet.2012.10.130.

    • Peer Reviewed
  • [Journal Article] Heterologously expressed ss- hydroxyl fatty acids froma metagenomic library of a marine sponge. Bioorg.2012

    • Author(s)
      R. He, T. Wakimoto, Y. Egami, H.Kenmoku, T. Ito, Y. Asakawa, I. Abe
    • Journal Title

      Med. Chem. Lett

      Volume: 22 Pages: 7322-7325

    • DOI

      DOI:10.1016/j.bmcl.2012.10.082

    • Peer Reviewed
  • [Journal Article] Porphyrins fromametagenomic library of the marine sponge Discodermia calyx.2012

    • Author(s)
      R. He, T. Wakimoto, Y. Takeshige, Y.Egami, H. Kenmoku, T. Ito, B. Wang, Y. Asakawa, I. Abe
    • Journal Title

      Mol. BioSyst.

      Volume: 8 Pages: 2334-2338

    • DOI

      DOI:10.1039/C2MB25169H

    • Peer Reviewed
  • [Journal Article] Calyxamides A and B, cytotoxic cyclic peptides fromthe marine sponge2012

    • Author(s)
      M. Kimura, T. Wakimoto, Y. Egami, K. C.Tan, Y. Ise, I. Abe
    • Journal Title

      Discodermia calyx. J. Nat. Prod.

      Volume: 75 Pages: 290-294

    • DOI

      DOI:10.1021/np2009187.

    • Peer Reviewed
  • [Journal Article] Labile natural products.2012

    • Author(s)
      T. Wakimoto, I. Abe
    • Journal Title

      MedChemComm

      Volume: 3 Pages: 866-870

    • DOI

      DOI:10.1039/C2MD20016C

    • Peer Reviewed
  • [Journal Article] Engineering of plant type III polyketide synthases.2012

    • Author(s)
      T. Wakimoto, H. Morita, I. Abe
    • Journal Title

      Methods in Enzymology

      Volume: 515 Pages: 337-358

    • DOI

      DOI:10.1016/B978-0-12-394290-6

    • Peer Reviewed
  • [Presentation] Calyculin A 生合成遺伝子ク ラスターの探索2012

    • Author(s)
      脇本敏幸
    • Organizer
      日本薬学会第 132 年会
    • Place of Presentation
      (札幌)シンポジウム
    • Year and Date
      2012-03-30
  • [Presentation] Search for the biosynthetic gene cluster of the cytotoxic polyketide calyculin A from the marine sponge Discodermia calyx2011

    • Author(s)
      脇本敏幸
    • Organizer
      University of Bristol
    • Place of Presentation
      University of Bristol (Bristol, UK)
    • Year and Date
      2011-11-22
  • [Presentation] Search for the biosynthetic gene cluster of the cytotoxic polyketide calyculin A from the marine sponge Discodermia calyx2011

    • Author(s)
      脇本敏幸
    • Place of Presentation
      University of Bonn (Bonn, Germany)
    • Year and Date
      2011-11-22
  • [Presentation] Search for the biosynthetic gene cluster of the cytotoxic polyketide calyculin A from the marine sponge Discodermia calyx2011

    • Author(s)
      脇本敏幸
    • Place of Presentation
      University of Tubingen (Tubingen, Germany)
    • Year and Date
      2011-10-27
  • [Presentation] Chemistry and biology of calyculin A2011

    • Author(s)
      脇本敏幸
    • Organizer
      The 6th Korea-Japan Young Scientists Symposium
    • Place of Presentation
      Seoul, Korea
    • Year and Date
      2011-06-24
  • [Remarks]

    • URL

      http://www.f.u-tokyo.ac.jp/~tennen/head.htm

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Published: 2014-09-25  

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