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New mechanisms by which statins lower plasma cholesterol
Journal of Lipid ResearchVol. 57Issue 8p1325–1326Published online: June 23, 2016- Henri Brunengraber
Cited in Scopus: 2The use of an enzyme inhibitor in vivo to lower a metabolic rate often results in the activation of the targeted enzymatic reaction. The dose of inhibitor is adjusted so that the desired effect is achieved and maintained in spite of the activation of the enzyme. After statins were developed in the 1970s to inhibit HMG-CoA reductase and lower plasma cholesterol, it was soon reported that these drugs induce a strong activation of the reductase (1). This was not a particular concern to clinicians because, in many patients, the dose of statin could be adjusted to keep the plasma concentration of cholesterol in a range that decreased the risk of myocardial infarction.