The Selectivity of Beauveriolide Derivatives in Inhibition toward the Two Isozymes of Acyl-CoA: cholesterol Acyltransferase

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概要

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• The selectivity of synthetic beauveriolide derivatives in inhibition toward the two isozymes of acyl-CoA: cholesterol acyltrasferase (ACAT), ACAT1 and ACAT2, was studied in cell-based assays using ACAT1- or ACAT2-expressing Chinese hamster ovary (CHO) cells. NBV274, 285 and 300 showed ACAT1 selective inhibition similar to that of natural beauveriolides I and III, NBV345 inhibited both isozymes with similar potency, but NBV281, 331 and 249 were found to selectively inhibit the ACAT2 isozyme. The structure-activity relationships indicated that a subtle structural difference in beauveriolide derivatives can affect the selectivity of inhibition of the ACAT isozymes.

• 公益社団法人日本薬学会の論文
• 2009-04-01

著者

• 外山 博英

  山口大学農学部生物機能科学科

• 外山 博英

  京大・化研:(現)山口大・農

• TAKAHASHI Takashi

  Department of General Medicine, Kanazawa Medical University

• MATSUDA Daisuke

  Graduate School of Pharmacy, Kitasato University

• OHSHIRO Taichi

  Graduate School of Pharmacy, Kitasato University

• TOMODA Hiroshi

  Graduate School of Pharmacy, Kitasato University

• Toyama Hirohide

  Department Of Biological Chemistry Faculty Of Agriculture Yamaguchi University

• Takayanagi H

  Research Center For Biological Function The Kitasato Institute

• SUNAZUKA Toshiaki

  Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato Uni

• NAGAI Kenichiro

  Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato Uni

• OMURA Satoshi

  Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato Uni

• Doi Takayuki

  Department Of Applied Chemistry Tokyo Institute Of Technology

• Doi Takayuki

  Department Of Applied Chemistry Graduate School Of Science And Engineering Tokyo Institute Of Techno

• Rudel Lawrence

  Atherosclerosis Research Program Wake Forest University School Of Medicine

• Hirose T

  School Of Pharmacy Kitasato University

• Nagai Kenichiro

  Kitasato Institute For Life Sciences And Graduate School Of Infection Control Sciences Kitasato Univ

• Tanaka Y

  School Of Pharmaceutical Sciences Kitasato University The Kitasato Institute

• Omura S

  Kitasato Institute For Life Sciences Kitasato University

• Sunazuka T

  信州大学医学部附属病院 薬剤部

• Sunazuka Toshiaki

  Kitasato Univ. Tokyo Jpn

• Sunazuka Toshiaki

  School Of Pharmaceutical Sciences Kitasato University:research Center For Biological Function The Ki

• Toyama Hirohide

  Institute For Chemical Research Kyoto University

• Tanaka Toshiaki

  Department Of Applied Chemistry Tokyo Institute Of Technology

• Omura Satoshi

  Kitasato Institute For Life Sciences And Graduate School Of Infection Control Sciences Kitasato Univ

• Tanaka H

  External Science Affairs Fujisawa Pharmaceutical Co. Ltd.

• Koyama Nobuhiro

  School Of Pharmacy Kitasato University

• Ohshiro Taichi

  Graduate School Of Pharmaceutical Sciences Kitasato University:(present Office)department Of Medhici

• Takahashi Takashi

  Department Of Applied Chemistry Tokyo Institute Of Technology

• Hirose Tomoyasu

  Kitasato Univ. Tokyo Jpn

• Takamatsu S

  Univ. Mississippi Ms Usa

• Matsuda Daisuke

  Graduate School Of Pharmaceutical Sciences Kitasato University

• Takahashi Takashi

  Department Of Applied Chemistry Graduate School Of Science And Engineering Tokyo Institute Of Techno

• Tomoda Hiroshi

  Graduate School Of Pharmaceutical Sciences Kitasato University

• Nonaka Kenichi

  Kitasato Institute For Life Sciences Kitasato University

• Ohshiro Taichi

  Graduate School Of Pharmaceutical Sciences Kitasato University

• Tomoda Hiroshi

  Graduate School Of Pharmaceutical Sciences Kitasato Univ.

• Sunazuka Toshiaki

  Kitasato Institute for Life Sciences and Graduate School of Infection Control Science, Kitasato University

• Tomoda Hiroshi

  Graduate School of Pharmaceutical Science, Kitasato University

• Omura Satoshi

  Kitasato Institute

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