HMG-CoA Reductase (HMGCR)
HMGCR (HMG-CoA reductase) is the rate-controlling enzyme of the mevalonate pathway, the metabolic pathway that produces cholesterol and other isoprenoids. Normally in mammalian cells this enzyme is suppressed by cholesterol derived from the internalization and degradation of low density lipoprotein (LDL) via the LDL receptor as well as oxidized species of cholesterol. Competitive inhibitors of the reductase induce the expression of LDL receptors in the liver, which in turn increases the catabolism of plasma LDL and lowers the plasma concentration of cholesterol, an important determinant of atherosclerosis. This enzyme is thus the target of the widely available cholesterol-lowering drugs known collectively as the statins. HMGCR is anchored in the membrane of the endoplasmic reticulum, and was long regarded as having seven transmembrane domains, with the active site located in a long carboxyl terminal domain in the cytosol.
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Lovastatin (洛伐他汀) 是高效HMG-CoA还原酶抑制剂，IC50为3.4 nM，有降血脂作用。
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Simvastatin (Zocor)是HMG-CoA还原酶的竞争性抑制剂，Ki为0.1-0.2 nM。
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Fluvastatin sodium (XU62-320) is a potent, water-soluble inhibitor of HMG-CoA reductase, widely used as a cholesterol- lowering drug. Fluvastatin sodium 是HMG-CoA还原酶竞争性抑制剂。
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Pravastatin sodium, a hydrophilic inhibitor, inhibits HMG-CoA reductase resulting in the reduction of cholesterol synthesis. Pravastatin sodium是HMG-CoA还原酶抑制剂，对甾醇合成的IC50为5.6 μM。
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Atorvastatin calcium, a hydrophilic inhibitor, inhibits the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Atorvastatin hemicalcium salt 是高活性HMG-CoA还原酶抑制剂，IC50为8 nM。
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