HMGCR
HMGCR (3-hydroxy-3-methylglutaryl-CoA reductase, also written HMG-CoA reductase) is the rate-limiting enzyme of cholesterol and isoprenoid synthesis. It converts HMG-CoA to mevalonic acid and is the main target of statin drugs. Browse Assay Genie's current range of HMGCR research reagents below, or read on for the biology behind the target.
HMGCR catalyses the conversion of (3S)-hydroxy-3-methylglutaryl-CoA (HMG-CoA) to mevalonic acid. This is the rate-limiting step in the synthesis of cholesterol and other isoprenoids, so the enzyme plays a critical role in cellular cholesterol homeostasis. The protein is a member of the HMG-CoA reductase family and is assigned to the oxidoreductase gene group.
Activity is controlled by negative feedback. Sterols and non-sterol metabolites derived from mevalonate, the product of the reaction, regulate the enzyme. In mammalian cells HMGCR is normally suppressed by cholesterol delivered through internalisation and degradation of low density lipoprotein (LDL) via the LDL receptor. Competitive inhibitors of the reductase induce LDL receptor expression in the liver, which increases the catabolism of plasma LDL and lowers plasma cholesterol, an important determinant of atherosclerosis. The HMGCR protein localises to the endoplasmic reticulum membrane and the peroxisome membrane.
HMGCR is the main target of statins, a class of cholesterol-lowering drugs, which makes the HMGCR gene a central subject in lipid metabolism and cardiovascular research. Alternatively spliced transcript variants encoding different isoforms have been reported. Mouse and rat each carry an orthologous Hmgcr gene, allowing the enzyme to be studied in common rodent models.
HMGCR catalyses the rate-limiting step of cholesterol and isoprenoid synthesis, making it a key readout of flux through the mevalonate pathway.
As the main target of statins, HMGCR is central to studies of cholesterol-lowering drugs and competitive inhibition of the reductase.
Sterols and mevalonate-derived metabolites suppress the enzyme by negative feedback, a mechanism studied in cellular cholesterol homeostasis.
Reductase inhibition raises hepatic LDL receptor expression and lowers plasma cholesterol, an important determinant of atherosclerosis.
HMGCR converts HMG-CoA to mevalonic acid, the rate-limiting step in the synthesis of cholesterol and other isoprenoids. It therefore plays a critical role in cellular cholesterol homeostasis and is the main target of statins, a class of cholesterol-lowering drugs.
HMGCR is the HGNC symbol for 3-hydroxy-3-methylglutaryl-CoA reductase, commonly called HMG-CoA reductase. The enzyme carries the EC number 1.1.1.34. Alternatively spliced transcript variants encoding different isoforms have been found for this gene.
Yes. Mouse and rat both have an orthologous gene named Hmgcr. Researchers often use rodent models for cholesterol metabolism work, but check the datasheet of any product for its validated reactivity.
Other cholesterol-metabolism enzymes, LDL receptor pathway proteins and lipid markers with products at Assay Genie.
Gene and protein annotations from HGNC, NCBI Gene and UniProt P04035; product specifications from Assay Genie datasheets.