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Agents affecting lipid metabolism. XXVI. Specificity of some inhibitors of the late stages of cholesterol biosynthesis

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Lipids

Abstract

The capacity of 22,25-DAC, AY-9944 and triparanol to inhibit cholesterol biosynthesis from three precursors, mevalonate, 7-dehydrocholesterol and desmosterol, has been studied in rat liver homogenates.

Evidence is presented that, in vitro, 22,25-DAC, a potent inhibitor of the sterol Δ24-reductase, also inhibits the 7-dehydrocholesterol-Δ7-reductase system.

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Abbreviations

22,25-DAC (SC-11952):

20α-(2-dimethylaminoethyl)amino-5α-pregnan-3β-ol dihydrochloride

AY-9944:

trans-1,4-bis (2-chlorobenzylaminomethyl)cyclohexane dihydrochloride triparanol (Mer-29), 1-[p-(β-diethylaminoethoxy)phenyl]-1-(p-tolyl)-2-(p-chlorophenyl) ethanol

20,25-DAC (SC-12937):

N-methyl-N-(3-dimethylamino) propyl-17β-aminoandrost-5-en-3β-ol

Δ7-reductase:

7-dehydrocholesterol-Δ7-reductase

Δ24-reductase:

24-dehydrosterol-Δ24-reductase

MVA:

mevalonic acid

HMGCoA:

hydroxymethylglutarylcoenzyme A

DBED:

N,N′-dibenzylethylenediamine

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Authors and Affiliations

  1. Department of Biochemistry, Ayerst Research Laboratories, Montreal, Canada

    M. Kraml, J. Dubuc & D. Dvornik

Authors
  1. M. Kraml
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  2. J. Dubuc
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  3. D. Dvornik
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Kraml, M., Dubuc, J. & Dvornik, D. Agents affecting lipid metabolism. XXVI. Specificity of some inhibitors of the late stages of cholesterol biosynthesis. Lipids 2, 5–7 (1967). https://doi.org/10.1007/BF02531992

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  • DOI: https://doi.org/10.1007/BF02531992

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