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analysis
use of inhibitor K-604, selective for isoform ACAT-1, to measure the individual enzymatic activities of isoforms ACAT-1 and ACAT-2 in semniferous tubule
drug development
regulation of ACAT1 activities in hepatic stellate cells can be a target for treatment of liver fibrosis
drug development
regulation of ACAT1 activities in hepatic stellate cells can be a target for treatment of liver fibrosis
drug development
selective inhibitors of the cholesterol esterifying enzyme sterol-O acyltransferase 2 (SOAT2) hold great promise as effective atherosclerotic cardiovascular disease therapeutics
drug development
the enzyme is a potential target for treating hypercholesterolemia
drug development
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the enzyme is regarded as a potential therapeutic target for cardiovascular diseases
drug development
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regulation of ACAT1 activities in hepatic stellate cells can be a target for treatment of liver fibrosis
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medicine
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identified as a major target for inhibition, based on the hypothesis that enzyme inhibitors may have a direct antiatherosclerotic effect within the arterial wall and a direct effect in blocking cholesterol absorption in the small intestine, and in reducing very-low-density lipoprotein secretion in the hepatocytes
medicine
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for both isoform ACTA1 and ACAT2, overexpression in rat hepatoma McA-RH7777 cells results in increased synthesis, cellular accumulation, and secretion of cholesteryl esters. This leads to decreased intracellular degradation and increased secretion of very low density liporotein apoB. Overexpression of ACAT2 has significantly greater impact upon assembly and secretion of very low density liporotein from liver cells than that of ACAT1
medicine
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inbred strains with high/low response in low-density lipoprotein cholesterol to dietary cholesterol and fat, resp. High responding animals have significantly higher percent cholesterol absorption, hepatic free and esterified cholesterol, and hepatic enzyme activity than low responding animals on high cholesterol and high fat diet. Hepatic enzyme activity, but not the intestinal activity is associated with hepatic cholesterol concentration and percent cholesterol absorption
medicine
elevated ACAT2expression may serve as a new biomarker for certain forms of hepatocellular carcinoma
medicine
hepatic ACAT2 plays a critical role in driving the production of atherogenic lipoproteins, and therapeutic interventions, such as the ACAT2-specific antisense oligonucleotide used here, which reduce acyltransferase 2 (ACAT2) function in the liver without affecting ACAT1, may provide clinical benefit for cardiovascular disease prevention
medicine
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systemic ACAT inhibition reduces circulating tumor necrosis factor-alpha levels in hypercholesterolemic subjects and improves resistance-vessel endothelial function, with small effects on circulating cholesterol. This may be a novel therapeutic strategy to target vascular inflammation and endothelial dysfunction in atherosclerosis
medicine
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ACAT is a key enzyme in controlling cholesterol metabolism and represents a promising target for the development of therapeutic agents and inhibitors to control hypercholesterolemia, atherosclerosis and Alzheimer's disease
medicine
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an anti-oxidative ACAT inhibitor or the combination of an antioxidant and an ACAT inhibitor protects foam cells from oxidative stress and effectively reduces cholesterol levels, which would be a promising approach in anti-atherosclerotic therapy
medicine
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statin treatment reduces ACAT2 activity in human liver and this effect, in combination with a reduced ApoE expression, may contribute to the favorable lowering of VLDL cholesterol seen in addition to the LDL lowering during statin treatment
medicine
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the results suggest that the ACAT inhibitor VULM 1457 is a prospective hypolipidemic and anti-atherogenic drug which treats diabetes
medicine
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the results suggest that this novel hypolipidaemic agent exert antiarrhythmic and infarct size-limiting effects in the diabetic-hypercholesterolaemic rat heart
medicine
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the study provides evidence that purified esculeogenin A significantly suppresses the activity of ACAT protein and leads to reduction of atherogenesis
medicine
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the study provides evidence that purified esculeogenin A significantly suppresses the activity of ACAT protein and leads to reduction of atherogenesis
medicine
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feeding a diet suplemented with linoleic acid, conjugated linoleic acid, alpha-linolenic acid or conjugated linolenic acid results in decrease in plasma cholesterol, with conjugated linoleic acid being the most effective. Diets have no effect on sterol regulatory element binding protein-2, liver X receptor, 3-hydroxy-3-methylglutary-CoA reductase, LDL receptor, and cholesterol-7-hydroxylase. The four octadecaenoic acids increase the excretion of fecal neutral sterols with conjugated linoleic acid being most effective followed by alphga-linolenic acid, linoleic acid and conjugated linolenic acid. Dietary conjugated linoleic acid is associated with the least intestinal acyl coenzyme A: cholesterol acyltransferase activity followed by alpha-linolenic acid, linoleic acid and conjugated linolenic acid in a decreasing trend
medicine
a panel of ovarian cancer cell lines (OC-314, SKOV-3 and IGROV-1) displays significant increase in the expression of ACAT1 and cholesterol ester levels compared to primary ovarian epithelial cells. ACAT1 knockdown ovarian cancer cell lines show significant suppression of cell proliferation, migration and invasion compared to their respective controls. ACAT-1 inhibition enhances apoptosis with a concurrent increase in caspases 3/7 activity and decreased mitochondrial membrane potential, and ACAT1-inhibited ovarian cancer cell lines display enhanced chemosensitivity to cisplatin treatment
medicine
treatment of 63 patients with metastatic adrenocortical carcinoma with oral nevanimibe at doses ranging from 1.6 mg/kg/day to 158.5 mg/kg/day. No patients experienced a complete or partial response. 13 of 48 (27%) patients who underwent imaging at 2 months had stable disease, and 4 of these had stable disease for more than 4 months
nutrition
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increase in enzyme activity in animals fed with palmitic acid. No difference in hepatic enzyme activity in animals fed with oleic acid or linoleic acid
nutrition
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feeding a diet suplemented with linoleic acid, conjugated linoleic acid, alpha-linolenic acid or conjugated linolenic acid results in decrease in plasma cholesterol, with conjugated linoleic acid being the most effective. Diets have no effect on sterol regulatory element binding protein-2, liver X receptor, 3-hydroxy-3-methylglutary-CoA reductase, LDL receptor, and cholesterol-7-hydroxylase. The four octadecaenoic acids increase the excretion of fecal neutral sterols with conjugated linoleic acid being most effective followed by alphga-linolenic acid, linoleic acid and conjugated linolenic acid. Dietary conjugated linoleic acid is associated with the least intestinal acyl coenzyme A: cholesterol acyltransferase activity followed by alpha-linolenic acid, linoleic acid and conjugated linolenic acid in a decreasing trend
pharmacology
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ACAT-1 and ACAT-2 selective inhibitors may prove to have clinical benefit to reduce atherosclerosis via directly reducing the size of the lipid-rich core in the atherosclerotic plaques or the absorption of cholesterol in intestine, respectively
pharmacology
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K-604, a potent and selective inhibitor of ACAT-1, suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels, providing direct evidence that pharmacological inhibition of ACAT-1 in the arterial walls leads to suppression of atherosclerosis
pharmacology
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the data suggest that antiatherosclerotic activity of licorice in hypercholesterolemic patients might be related with its ACAT inhibitory effects
pharmacology
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the data suggest that antiatherosclerotic activity of licorice in hypercholesterolemic patients might be related with its ACAT inhibitory effects
pharmacology
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the results strongly support the idea that CS-505 could be promising as a therapeutic agent for the treatment of atherosclerosis