3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA reductase) catalyzes the rate limiting step in cholesterol biosynthesis - conversion of 3-hydroxy-3-methyl-glutaryl-CoA to mevalonic acid. HMG-CoA reductase is a transmembrane enzyme, bound to endoplasmic reticulum.
HMG-CoA Reductase Inhibitors |
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Cat. No. | Product Name / Activity |
3309 | Fluvastatin sodium |
Potent HMG-CoA reductase inhibitor | |
1530 | Lovastatin |
Potent HMG-CoA reductase inhibitor | |
1526 | Mevastatin |
HMG-CoA reductase inhibitor | |
4942 | Pitavastatin calcium |
HMG-CoA reductase inhibitor | |
2318 | Pravastatin sodium salt |
HMG-CoA reductase inhibitor | |
6343 | Rosuvastatin calcium |
Potent HMG-CoA reductase inhibitor | |
1965 | Simvastatin |
HMG-CoA reductase inhibitor | |
Other |
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Cat. No. | Product Name / Activity |
2969 | SR 12813 |
Enhances HMG-CoA reductase degradation. Also PXR agonist |
3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA reductase) catalyzes the rate limiting step in cholesterol biosynthesis - the conversion of 3-hydroxy-3-methyl-glutaryl-CoA into mevalonic acid. This transmembrane enzyme is bound to the endoplasmic reticulum and is ubiquitously expressed.
When cholesterol levels falls, HMG-CoA reductase is transcriptionally upregulated by sterol regulatory element binding protein (SREBP), which binds to the sterol regulatory element (SRE) in the 5' region of the HMG-CoA gene. When cholesterol levels are elevated, short-term regulation of HMG-CoA is mediated by Ser872 phosphorylation by AMP-activated protein kinase and long-term regulation is mediated by the increased sensitivity of this enzyme to proteolytic breakdown. HMG-CoA reductase is the pharmalogical target for statins and the human gene encoding this enzyme is localized to 5q13.3-q14.
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