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Journal of Lipid Research, Vol. 2, 258-262, July 1961
Copyright © 1961 by Lipid Research, Inc.

Effect of mevalonate analogues upon cholesterol biosynthesis

Herbert Weiss , Elliott Schiffmann , and Elwood Titus

Laboratory of Chemical Pharmacology, National Heart Institute, National Institutes of Health, Bethesda 14, Maryland

Three analogues of mevalonic acid have been found to inhibit cholesterol biosynthesis in liver homogenates in the following order of efficacy: 3-methyl-3-hydroxy pentanoic acid > Dgr2-3-methyl pentenoic acid > Dgr3-3-methyl pentenoic acid. The hydroxy acid produces half the maximum inhibition at a concentration of 5 µmoles/ml of homogenate. This corresponds to a ratio of 100 µmoles of inhibitor to 1 µmole of substrate.

Submitted on October 28, 1960


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