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Berndt, J. ; Gaumert, R. ; Still, J.S.

Mode of action of the lipid-lowering agents, elofibrate and BM 15075, on cholesterol biosynthesis in rat liver.

Atherosclerosis 30, 147-152 (1978)

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Open Access Green as soon as Postprint is submitted to ZB.

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When rats were fed a diet containing 0.3% clofibrate or a derivative of this drug, BM 15075, serum cholesterol was lowered within 3-7 days by 26-38%. Both drugs diminished the activity of hydroxymethylglutaryl CoA reductase, the regulatory enzyme of hepatic cholesterol biosynthesis, in rat liver microsomes by about 60% under the same conditions. The decrease in the activity of the enzyme obviously is due to changes in the amount of enzyme protein. Under in vitro conditions, microsomal hydroxymethylglutaryl CoA reductase was inhibited competitively by (1.35 mM) clofibrate acid (sodium salt) and by BM 15075 (1 mM) with respect to its substrate. These results give evidence that these drugs can affect both, the rate of synthesis and the substrate affinity of hydroxymethylglutaryl CoA reductase.

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Publication type Article: Journal article

Document type Scientific Article

Corresponding Author

ISSN (print) / ISBN 0021-9150

e-ISSN 1879-1484

Journal Atherosclerosis

Quellenangaben Volume: 30, Issue: 2, Pages: 147-152

Publisher Elsevier

Publishing Place Amsterdam

Non-patent literature Publications

Reviewing status Peer reviewed

Institute(s) Institut für Biochemie