Which drug belongs to the class 3 hydroxy 3 Methylglutaryl CoA?
3-Hydroxy-3-methylglutaryl–coenzyme A (HMG-CoA) reductase inhibitors (statins) are among the most prescribed medications in the United States. Statins act on the rate-limiting step in cholesterol biosynthesis (the conversion of HMG-CoA to mevalonate) and are effective in treating dyslipidemia.
What is the substrate of 3 hydroxy 3 Methylglutaryl CoA reductase?
The structure of statins is similar to 3-hydroxy-3-methylglutaryl-CoA, the native substrate of HMG-CoA reductase. They are mainly used as cholesterol-lowering drugs. There are two main types of statins: synthetic and naturally derived.
What does HMG-CoA bind to?
In human HMGR, the catalytic lysine is found on the monomer that binds the HMG-CoA and comes from the so-called cis-loop (a section that connects the HMG-CoA-binding region with the NADPH-binding region).
What reaction does HMG-CoA reductase catalyse?
HMG-CoA reductase catalyses the NADPH-dependent reduction of HMG-CoA to mevalonic acid (MVA in Figure 2). It is considered to be the rate-limiting enzyme of the cholesterol biosynthetic pathway. Thus, changes in the activity of the enzyme are paralleled by changes in cholesterol synthesis.
Which drug belongs to the class 3 hydroxy 3 methylglutaryl coenzyme A HMG-CoA reductase inhibitors quizlet?
Atorvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.
Which drug decreases cholesterol synthesis by inhibiting the enzyme 3 hydroxy 3 methylglutaryl coenzyme A reductase?
Statins. Statins, as 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors, are normally used as first-line agents for hypercholesterolemia, especially for those patients who have fasting triglycerides less than 500 mg/dL.
Which of the following drug decreases cholesterol synthesis by inhibiting the enzyme 3 hydroxy 3 methylglutaryl coenzyme A reductase?
Inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase commonly known as statins are widely used for treating hypercholesterolemia. However, there is much evidence to suggest that statins may have other properties in addition to their cholesterol-lowering effect.
What is the role of HMG-CoA reductase?
Function. HMG-CoA Reductase (or 3-hydroxy-3-methyl-glutaryl-CoA reductase or HMGR) is the rate-controlling enzyme of the mevalonate pathway, responsible for cholesterol and other isoprenoid biosynthesis. HMGR is a transmembrane protein, containing 8 domains, that is anchored in the membrane of the endoplasmic reticulum …
Which of the following drug decreases cholesterol synthesis by inhibiting the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase?
Which drug belongs to the class 3-hydroxy-3-methylglutaryl coenzyme A HMG-CoA reductase inhibitors quizlet?
What is the mechanism of action for beta hydroxy beta methylglutaryl coenzyme A HMG-CoA reductase inhibitors?
β-Hydroxy β-methylglutaryl-CoA (HMG-CoA) reductase inhibitors, more popularly known as statins, work by reducing the cholesterol levels in the body. HMG-CoA inhibitors interfere with the ability of the body to build cholesterol from dietary fat.
Which amino acid is involved in binding of HMG-CoA reductase?
a C-terminal catalytic domain (amino acid interval: 489-871), namely the 3-hydroxy-3-methyl-glutaryl-CoA reductase domain. This domain is required for the proper enzymatic activity of the protein.
How do you convert HMG-CoA to mevalonate?
HMG-CoA is reduced to mevalonate by NADPH. This is the rate limiting step in cholesterol synthesis, which is why this enzyme is a good target for pharmaceuticals (statins). Mevalonate is phosphorylated at the 5-OH position to yield mevalonate-5-phosphate (also called phosphomevalonic acid).
What happens when HMG-CoA reductase inhibitors?
HMG coenzyme-A reductase inhibitors Lower intracellular cholesterol concentrations cause over-expression of the LDL receptor in the plasma membrane of hepatocytes. This overexpression increases the clearance of circulating LDL, reducing plasma concentrations of LDL cholesterol.
Where does HMG-CoA bind to HMG-CoA reductase How do you know?
HMG-CoA reductase 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.