Inhibition of Acyl Coenzyme A : Cholesterol Acyltransferase by 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase Inhibitors

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概要

• 論文の詳細を見る

• Relatively high concentrations of MK-733 (simvastatin) and MK-803 (lovastatin, mevinolin), which are 3-hydroxy-3-methylglutary coenzyme A (HMG-CoA) reductase inhibitors, were found to inhibit acyl coenyme A : cholesterol acyltransferase (ACAT) of rabbit intestial microsomes with IC_<50>'s of 2.0 × 10^<-5> and 3.6 ×10^<-5>M, respectively. Dihydroxy acid forms of both MK-733 and MK-803 did not inhibit ACAT activity. A kinetic analysis using a Lineweaver-Burk plot indicated that MK-733 is a competitive inhibitor of ACAT, with a K_i value of 1.2 ×10^<-5>M.

• 社団法人日本薬学会の論文
• 1989-06-25

著者

• 石田 史明

  Central Research Laboratories, Banyu Pharmaceutical Co., Ltd.,

• 亀井 敏夫

  Central Research Laboratories, Banyu Pharmaceutical Co., Ltd.,

• 佐藤 昭子

  Central Research Laboratories, Banyu Pharmaceutical Co., Ltd.

• 飯塚 ゆり

  Central Research Laboratories, Banyu Pharmaceutical Co., Ltd.

• 飯塚 ゆり

  Central Research Laboratories Banyu Pharmaceutical Co. Ltd.

• 佐藤 昭子

  Central Research Laboratories Banyu Pharmaceutical Co. Ltd.

関連論文

• Effect of Bacteriohopane-32-ol on Lipid Metabolism in Hep G2 Cells
• Effect of an Inhibitor of Squalene Epoxidase, NB-598,on Lipid Metabolism in Hep G2 Cells
• Inhibition of Acyl Coenzyme A : Cholesterol Acyltransferase by 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase Inhibitors
• Enzymatic Properties of Squalene Epoxidase from Saccharomyces cerevisiae

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