Application

The HMGR activity kit is designed for the detection of HMG-CoA reductase activity. A major function of the kit is to screen for various inhibitors and activators of the purified catalytic subunit of the enzyme, HMG-CoA reductase, which may play a crucial role in therapeutics. The assay is based on the spectrophotometric measurement of the decrease in absorbance at 340 nm, which represents the oxidation of NADPH by the catalytic subunit of HMGR in the presence of the substrate HMG-CoA.

Biochem/physiol Actions

HMGR (3-hydroxy-3-methylglutaryl-CoA reductase) is a transmembrane glycoprotein located on the endoplasmic reticulum. This enzyme catalyzes the four-electron reduction of HMG-CoA to coenzyme A (CoA) and mevalonate, which is the rate-limiting step in sterol biosynthesis. The activity of HMGR is controlled through synthesis, degradation, and phosphorylation in order to maintain the concentration of mevalonate derived products. In addition to the physiological regulation of HMGR, the human enzyme has been targeted successfully by drugs in the clinical treatment of high serum cholesterol levels. Controlling serum cholesterol levels has an important therapeutic role since hypercholesterolemia often leads to the development of atherosclerosis and subsequently to cardiovascular pathologies, which might result in myocardial infarction and stroke. It has been suggested that a disturbance of cholesterol homeostasis contributes to the development of a chronic inflammatory state.

General description

The HMG-CoA Reductase Assay Kit is an important tool for the basic research of cholesterol and other relelated metabolic pathways.