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Statins and cholesterol synthesis

Statins and cholesterol synthesis
Inhibition of HMG CoA reductase reduces intracellular cholesterol levels; this activates a protease, which in turn cleaves SREBPs from the endoplasmic reticulum. The SREBPs translocate to the nucleus where they upregulate expression of the LDL receptor gene. Enhanced LDL receptor expression increases receptor-mediated endocytosis of LDL and thus lowers serum LDL. Inhibition of HMG CoA reductase also reduces intracellular levels of isoprenoids, which are intermediates in cholesterol biosynthesis.
HMG: hydroxymethylglutaryl; LDL: low-density lipoprotein; LDLR: LDL receptor; SRE: sterol regulatory element; SREBP: SRE binding proteins.
Reprinted with permission from: Vaughan, CJ, Gotto, AM, Basson, CT. J Am Coll Cardiol 2000; 35:1. Copyright © 2000 American College of Cardiology.
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