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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Naringenin, a common dietary flavonoid abundantly present in fruits and vegetables, is believed to possess strong anti-proliferative properties and the ability to induce apoptosis in hepatoma cell lines.
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Mevastatin (Compactin; ML236B)抑制HMG-CoA还原酶（HMGCR），可抑制类异戊二烯的生物合成，阻断蛋白的异戊二烯化，降低血浆胆固醇水平。
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Rosuvastatin Calcium是一种竞争性HMG-CoA还原酶抑制剂， with IC50为11 nM。
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Clinofibrate抑制hydroxymethylglutaryl coenzyme A reductase (HMGCR)（羟甲基戊二酰辅酶A还原酶），IC50为0.47 mM，是一种降脂剂，用于控制血液中的高胆固醇和甘油三酯水平。
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