Cholesterol synthesis inhibitor

    • Effect of a new inhibitor of cholesterol biosynthesis (AY 9944) on ...

      ABSTRACT AY 9944 is a novel inhibitor of cholesterol bio- synthesis which appears to act on the A7-reductase enzyme, interfering with the conversion of 7-dehydrocholesterol to cholesterol. In all tissues studied, with the exception of the lens, there was a reduction in cholesterol and a marked accumula- tion of 7-dehydrocholesterol. Isotope ...


    • [PDF File]EFFECT OF CHOLESTEROL SYNTHESIS INHIBITION IN NORMOCHOLESTEREMIC YOUNG MEN

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      of endogenous cholesterol synthesis as a means of reducing the cholesterol content of the body has been reviewed (1). One such specific inhibitor is the metal vanadium. Salts of vanadium have been shown to inhibit the utilization of mevalonic acid for cholesterol biosynthesis (2), to inhibit cholesterol biosynthesis in vitro andinvivo (3), to


    • Selective inhibition of cholesterol synthesis in liver versus ...

      Cholesterol synthesis inhibition was also measured us- ing dog liver tissue slices (0.2 mm thickness, 25 mg wet wt) (18). Slices were randomized for assay of inhibitors in 1.0 ml of the buffer described for hepatocytes. After a 10- min preincubation, cholesterol synthesis was assayed in duplicate by incorporation of [l-"C]acetate (1.8


    • [PDF File]RESEARCH ARTICLE Open Access MicroRNA-33a regulates cholesterol ...

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      treatment with both TGF-β1 and miR-33a inhibitor or TGF-β1 and miR-33a mimic was assessed by Western blot analysis. Furthermore, we evaluated the effect of miR-33a mimic and miR-33a inhibitor onSmad7,anegative ... cesses—cholesterol synthesis and cholesterol efflux—are deregulated and contribute to OA pathogenesis. How-ever, so far, the ...


    • Lovastatin, an inhibitor of cholesterol synthesis, induces

      ABSTRACT Lovastatin is a potent competitive inhibitor of the rate-limiting enzyme of cholesterol synthesis, 3-hydroxy-3-methylglutaryl-coenzyme A reductase (NADPH) [HMG-CoA reductase; (S)-mevalonate:NADP+ oxidoreductase (CoA-acyl-ating), EC 1.1.1.34]. We determined the subcelHular distribu-tion of HMG-CoA reductase at high resolution by means of


    • Expression of sterol regulatory element-binding protein 1c (SREBP-1c ...

      by feeding a diet containing a cholesterol synthesis inhibitor (lovastatin) and a bile acid binding resin (colestipol), the amount of nuclear SREBP-2 increased. This is the same response that is observed in cultured nonhepatic cells, and it leads to increased transcription of the genes encoding the cholesterol biosynthetic


    • Cholesterol sulfate is a naturally occurring inhibitor of ...

      THE JOURNAL OF BIOLOGICAL CHEMISTRY 0 1989 by The American Society for Biochemistry and Molecular Biology, Inc. Vol. 264, No. 13, Ieaue of May 5, pp. 7222-7227.1989 Printed in U.S.A. Cholesterol Sulfate Is a Naturally Occurring Inhibitor of Steroidogenesis in Isolated Rat Adrenal Mitochondria*


    • Effect of a novel squalene epoxidase inhibitor, NB-598, on the ...

      598 is a specific inhibitor of mammalian squalene epoxidase.2 Therefore, NB-598 is thought to be a useful tool for studying the regulation of cholesterol synthesis. To investigate the regulatory mechanism of cholesterol metabolism, we examined the effects of NB-598 on HMG- CoA reductase activity, LDL receptor activity, and squalene


    • Cholesterol Synthesis and Nerve Regeneration - University of Michigan

      by the cholesterol synthesis inhibitor, 20,25-diazacholes- terol. The inhibition of growth could be overcome by ad- dition of mevalonolactone, but not cholesterol, to the me- dium. Intraperitoneal administration of 200 nmol of dia- zacholesterol resulted in 92-98% inhibition of retinal cholesterol synthesis and accumulation of labeled des-


    • Inhibition of cholesterol biosynthesis by squalene epoxidase inhibitor ...

      cholesterol biosynthesis pathway, squalene epoxidase (EC 1.14.99.7), was generated as a target for the inhibi- tion of cholesterol biosynthesis (8,9). This enzyme cata- lyzes the oxidation of squalene to 2,30xidosqualene in the middle stage of the cholesterol biosynthesis path- way. Squalene epoxidase is located downstream of the


    • A Cholesterol Biosynthesis Inhibitor Blocks

      A Cholesterol Biosynthesis Inhibitor Blocks Staphylococcus aureus Virulence Chia-I Liu,1,2,3* George Y. Liu,4* Yongcheng Song,5* Fenglin Yin,6 Mary E. Hensler,7 Wen-Yih Jeng,1,2 Victor Nizet,7,8† Andrew H.-J. Wang,1,2,3† Eric Oldfield5,6† Staphylococcus aureus produces hospital- and community-acquired infections, with


    • Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional ...

      Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional activity of human estrogen and androgen receptor BENfORd MAfUVAdzE, YAYUN LIANG and SALMAN M. HYdER department of Biomedical Sciences and dalton Cardiovascular Research Center, University of Missouri, Columbia, MO 65211, USA Received May 6, 2014; Accepted June 18, 2014


    • Mevinolin: A Highly Potent Competitive Inhibitor of ...

      mevinolinate was an active inhibitor of cholesterol synthesis in an acute assay (50% inhibitory dose = 46 gg/kg). Further-more, it was shown that mevinolin was an orally active choles-terol-lowering agent in the dog. Treatment of dogs for 3 weeks with mevinolin at 8 mg/kg per day resulted in a 29.3 - 2.5% lowering of plasma cholesterol.


    • [PDF File]The TBK1/IKKε inhibitor amlexanox improves dyslipidemia and prevents ...

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      assaying serum 14C radioactivity 2 hrs after gavage of cold cholesterol mixed with 14C-cholesterol. These data demonstrated that amlexanox did not affect cholesterol absorption (Figure 2C). Because liver is the major site of cholesterol synthesis, we also examined hepatic cholesterol synthesis rate in response to amlexanox administration.


    • Lung Cancer Cells Survive Epidermal Growth Factor Receptor Tyrosine ...

      that lovastatin induced cholesterol depletion from lipid rafts and was able to restore sensitivity to gefitinib in resistant cell lines. 20,21. Taken together, these studies highlight the poten-tial for a combination therapy targeting cholesterol synthesis along with EGFR inhibition. The lipid cholesterol, an essential component of plasma


    • [PDF File]Antihyperlipidemics – Apolipoprotein B Synthesis Inhibitors: lomitapide ...

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      Lomitapide is a microsomal triglyceride transfer protein inhibitor indicated as an adjunct to a low-fat diet and other lipid lowering treatments, including LDL apheresis where available, to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDLC)


    • Mevinolin, an Inhibitor of Cholesterol Synthesis, Induces mRNA for Low ...

      that mevinolin, an inhibitor of cholesterol synthesis, elevates the level of mRNA for the low density lipoprotein receptor in livers of hamsters and rabbits. In hamsters the maximal effect (3-fold increase) occurred at 0.1% mevinolin in the diet for 10 days. The same dose produced a maximal induction (10-fold) of


    • An unexpected link between fatty acid synthase and cholesterol ...

      ferentiation, and these cholesterol-rich macrophages are asso-ciated with a poor prognosis in atherosclerosis (15, 16), dem-onstrating that cholesterol metabolism is a key biosynthetic pathway in macrophages. Here we provide evidence for a biosynthetic link between fatty acid synthase and cholesterol synthesis. Our data sug-


    • [PDF File]INHIBITION OF CHOLESTEROL SYNTHESIS IN RATS by James R. Clark

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      Two examples of this type of inhibitor are Mer-29 and AY9944. ... used on later intermediates of cholesterol synthesis to the reduction of 3-hydroxy-3~methylglutaryl-CoA. This work uses various metabolites of 3-hydroxy~3-methylglutaryl-CoA to competitively inhibit the enzyme


    • [PDF File]Evaluation of Squalestatine 1 as an Enzyme Inhibitor for Lowering ...

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      a new enzyme to lower the cholesterol level in humans. Cholesterol is a biological molecule found in all mammalian cells’ membrane. This molecule is necessary for the cell survival and is an obligatory precursor in the synthesis of steroid hormones, lipoproteins and bile acids. Cholesterol is also essential for the transport of


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