Inhibition of cholesterol biosynthesis by fluorinated mevalonate analogues

The conversion of mevalonate to cholesterol in rat liver homogenates (IC50 = 0.01-1.0 mM) is inhibited by 6- (I), 6,6-di- (II), and 6,6,6-trifluoromevalonate (III), as well as 4,4-difluoromevalonate (IV). Addition of compound I, III, or IV to rat liver homogenates results in the accumulation of 5-ph...

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Veröffentlicht in:	Biochemistry (Easton) Jg. 26; H. 15; S. 4717
Hauptverfasser:	Reardon, J E, Abeles, R H
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 28.07.1987
Schlagworte:	Animals Carboxy-Lyases - antagonists & inhibitors Carboxy-Lyases - isolation & purification Cholesterol - biosynthesis Hydrocarbons, Fluorinated - pharmacology Kinetics Liver - metabolism Male Mevalonic Acid - analogs & derivatives Phosphorylation Rats Rats, Inbred Strains Structure-Activity Relationship
ISSN:	0006-2960
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