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  • An antilipidemic agent based on the carbon skeleton of cholesterol. Colestolone targets sterol regulatory element binding protein (SREBP) which reduces the transcription of the 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR) gene, the rate-limiting enzyme in the sterol pathway. Colestolone is also metabolized by cells into polar sterols, which are known to inhibit HMGCR enzymatic activity.
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