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2002 Fiscal Year Final Research Report Summary

Development of novel anti-atheroscleroic agents

Research Project

Project/Area Number 12557220
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section展開研究
Research Field 医薬分子機能学
Research InstitutionKumamoto University

Principal Investigator

NAKAYAMA Hitoshi  Kumamoto University, Graduate School of Medical and Pharmaceutical Sciences, Professor, 大学院・医学薬学研究部, 教授 (70088863)

Co-Investigator(Kenkyū-buntansha) KUNIYASU Akihiko  Kumamoto University, Graduate School of Medical and Pharmaceutical Sciences, Associate Professor, 大学院・医学薬学研究部, 助教授 (90241348)
MIYAZAKI Akira  Showa University, School of Medicine, Professor, 医学部, 教授 (70253721)
ISHIZUKA Tadao  Kumamoto University, Graduate School of Medical and Pharmaceutical Sciences, Associate Professor, 大学院・医学薬学研究部, 助教授 (60176203)
SANNO-HE Kunio  Mitsui Chemical Co., Institute for Material Sciences, Team Leader, マテリアルサイエンス研究所, 計算科学室長
NISHI Takao  Ohtsuka Pharmaceutical Co., Section of Medical Creation, Team Leader, 徳島第2工場・医薬生産部研究室, 室長
Project Period (FY) 2000 – 2002
Keywordssulfonylurea / glibenclamide / macrophage / CD36 / ACAT inhibitors / cholesterol metabolism / scavenger receptors
Research Abstract

We have found that glibendamide, a typical antidiabetic sulfonylurea, inhibits acyl CoA:cholesterol acyllransferase (ACAT) that plays a crucial role to esterify the intracellular free cholesterol and a trigger to form foamed cells in macrophage. In this project we aim to develop novel ACAT inhibitors that are distinct from conventional ones in chemical structures and properties, because the conventional drug candidates of chemically neutral in charge are worried about their adverse effects on adrenal grand. During the passed three years, we organized a team of bioorganic chemist, synthetic organic chemist, molecular pharmacologist, and professionals in in vivo evaluation of drugs, and incomputer-aided drug design. We are succeeded in creating several drug candidates that are eliminated inslin secrition activity and have unique characteristics for ACAT inhibition in term of selective deliverly to taget cells and organs. The compounds are preparing for the patents and we will open the detailed information after the patent issue is completed.

  • Research Products

    (12 results)

All Other

All Publications (12 results)

  • [Publications] A.Kuniyasu, et al.: "CD36-mediated endocytic uptake of AGE in mouse 3T3-L1 and human subcutaneous adipocytes"FEBS Lett.. 537. 85-90 (2003)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] H.Yoshikawa, et al.: "Photochemical identification of the binding region for (S)-semotiadil on sodium channels"Heterocycles. 59(2). 613-622 (2003)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] A.Miyazaki, et al.: "Scavenger receptors that recognize advanced glycation end products"Trends Cardiovasc.Med.. 12(6). 258-262 (2002)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] K.Kawahara, et al.: "Efficient identification of photolabeled amino acid by immuno-purification and mass spectrometry"Biochem. J.. 363(2). 223-232 (2002)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] A.Kuniyasu, et al.: "Adipocytes recognize and degrade oxidized LDL through CD36"Biochem.Biophys.Res.Commun. 295(2). 319-323 (2002)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] K.Kawahara, et al.: "Induction of CHOP and apoptosis by nitric oxide in p53-deficient microglial cells"FEBS Lett.. 506(2). 135-139 (2001)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Kuniyasu, et al.: "CD36-mediated endocytic uptake of AGE in mouse 3T3-L1 and human subcutaneous adipocytes."FEBS. Lett.. 537. 85-90 (2003)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] H. Yoshikawa, et al.: "Photochemical identification of the binding region for (s)-semotiadil on sodium channels."Heterocycles. 59(2). 613-622 (2003)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] A. Miyazaki, et al.: "Scavenger receptors that recognize advanced glycation end products."Trends Canliovasc. Med.. 12(6). 258-262 (2003)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] K. Kawahara, et al.: "Efficient identification of photolabeled amino acids by Immuno-purification and mass spectrometry."Biochem. J.. 363(39). 223-232 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] A. Kuniyasu, et al.: "Adipocytes recognize and degrade oxidized LDL through CD36."Biochem. Biophys. Res. Commun.. 295(2). 319-323 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] K. Kawahara, et al.: "Induction of CHOP and apoptosis by nitric oxide in P53-deflcient microglial cells."FEBS Lett.. 506(2). 135-139 (2001)

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 2004-04-14  

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