Statins

Natural Cholesterol Guide

Lower Cholesterol By Scott Davis

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Statins are the drugs most often prescribed to treat hypercholesterolaemia. The mechanism by which this class of drugs blocks cholesterol biosynthesis is competitive inhibition of HMG-CoA reductase (Fig. 2). This enzyme catalyses the rate-limiting

Fig. 2. Cholesterol biosynthesis. The rate-limiting step of this pathway is 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase activity. Statins competitively inhibit this enzyme. Intermediates from cholesterol biosynthesis are used as attachments to different proteins and enzymes. CoA, coenzyme A; PP, pyrophosphate

Fig. 2. Cholesterol biosynthesis. The rate-limiting step of this pathway is 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase activity. Statins competitively inhibit this enzyme. Intermediates from cholesterol biosynthesis are used as attachments to different proteins and enzymes. CoA, coenzyme A; PP, pyrophosphate step in cholesterol biosynthesis in the liver and other tissues. Indeed, statins bind to HMG-CoA reductase at nanomolecular concentrations. This leads to the displacement of the natural substrate (HMG-CoA), which itself binds at micromolar concentrations [73]. Blocking the enzyme leads to a significant reduction in plasma low-density lipoprotein (LDL) levels. In general, LDL levels are reduced by another 7% with each doubling of the dose [74]. However, it has become clear that lipid reduction alone cannot entirely account for the benefits of statin therapy.

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