• Search Research Projects
  • Search Researchers
  • How to Use
  1. Back to previous page

Structure activity relationship study of bile acid derivatives to development of novel vitamin D receptor ligand

Research Project

Project/Area Number 15K08018
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionTokyo Medical and Dental University

Principal Investigator

MASUNO Hiroyuki  東京医科歯科大学, 生体材料工学研究所, 技術専門職員 (80376714)

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: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
KeywordsビタミンD / 核内受容体 / 胆汁酸 / 構造活性相関 / ビタミンD
Outline of Final Research Achievements

To develop potent vitamin D receptor ligand which have no vitamin D skeleton and to investigate structure and activity relationships of lithocolic acid derivateves, I designed, synthesized and evaluated biological activity of novel lithocholic acid derivateves. I synthesized several lithocholic acid derivatives which have hydoxyl group containing alkyl group at carbon three on steroid skeleton. The vitamin D receptor activity of synthesized compounds were evaluated by differentiation-inducing activity in HL-60 human promyelocytic leukemia cell line. All of the compounds have higher activity than known lithocholic acid derivatives. The most potent compound have activity as well as 1,25-dihydroxyvitamin D3. These compounds have enough activities to use clinical application.

Report

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

    (5 results)

All 2017 2016 2015

All Presentation (5 results)

  • [Presentation] 高いビタミンD活性を有するリトコール酸誘導体の創製2017

    • Author(s)
      川崎波留, 佐々木晴江, 増野 弘幸, 河内恵美子, 石田寛明, 山本恵子, 影近弘之, 棚谷綾
    • Organizer
      日本薬学会第137年会
    • Place of Presentation
      仙台国際センター(宮城県仙台市)
    • Year and Date
      2017-03-24
    • Related Report
      2016 Research-status Report
  • [Presentation] リトコール酸をリード化合物にした新規ビタミン D 誘導体の創製2017

    • Author(s)
      川崎波留,佐々木晴江,増野弘幸,河内恵美子,影近弘之,棚谷綾
    • Organizer
      日本ビタミン学会第69回大会
    • Related Report
      2017 Annual Research Report
  • [Presentation] リトコール酸をリード化合物とした非セコステロイド型ビタミン D 誘導体の創製.2016

    • Author(s)
      川崎波留,佐々木晴江,増野弘幸,河内恵美子,影近弘之,棚谷綾
    • Organizer
      第34回メディシナルケミストリーシンポジウム
    • Place of Presentation
      つくば国際会議場(茨城県つくば市)
    • Year and Date
      2016-11-30
    • Related Report
      2016 Research-status Report
  • [Presentation] リトコール酸をリード化合物とした非セコステロイド型VDRリガンドの創製2016

    • Author(s)
      佐々木 晴江,増野 弘幸,河内 恵美子,影近 弘之,棚谷綾
    • Organizer
      日本薬学会第136年会
    • Place of Presentation
      パシフィコ横浜 (神奈川県・横浜市)
    • Year and Date
      2016-03-28
    • Related Report
      2015 Research-status Report
  • [Presentation] リトコール酸 3 位誘導体の合成とビタミン D 活性2015

    • Author(s)
      佐々木晴江,増野弘幸,数井優子,河内恵美子,影近弘之,棚谷綾
    • Organizer
      第33回メディシナルケミストリーシンポジウム
    • Place of Presentation
      幕張国際研修センター (千葉県・千葉市)
    • Year and Date
      2015-11-25
    • Related Report
      2015 Research-status Report

URL: 

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

Information User Guide FAQ News Terms of Use Attribution of KAKENHI

Powered by NII kakenhi