How do CETP inhibitors work?
How do CETP inhibitors work?
CETP inhibitors inhibit cholesterylester transfer protein (CETP), which normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL). Inhibition of this process results in higher HDL levels and reduces LDL levels.
What is a CETP?
Cholesteryl ester transfer protein (CETP) facilitates exchange of triglycerides and cholesteryl ester between high-density lipoprotein (HDL) and apolipoprotein B100–containing lipoproteins.
What is the function of CETP?
CETP is a hydrophobic glycoprotein that is secreted mainly from the liver and that circulates in plasma, bound mainly to HDL. It promotes the redistribution of cholesteryl esters, triglycerides, and, to a lesser extent, phospholipids between plasma lipoproteins.
Is CETP good or bad?
Since CETP activity can reduce HDL-cholesterol concentrations and CETP deficiency is associated with elevated HDL-cholesterol levels, CETP inhibitors have become a highly sought-after pharmacological target for the treatment of heart disease.
What is cholesteryl ester transfer protein inhibitors?
Cholesteryl ester transfer protein (CETP) inhibitors, including dalcetrapib, evacetrapib, and anacetrapib, are novel agents that have been developed to increase serum high-density lipoprotein cholesterol (HDL-c) concentration.
Is a statin?
Statins are a class of drugs often prescribed by doctors to help lower cholesterol levels in the blood. By lowering the levels, they help prevent heart attacks and stroke. Studies show that, in certain people, statins reduce the risk of heart attack, stroke, and even death from heart disease by about 25% to 35%.
What is BOD and COD in ETP?
BOD means Biochemical oxygen demand. The microorganisms use organic matter as a food source through oxidation which oxygen is consumed. COD, Chemical Oxygen Demand, is a measure of the total quantity of oxygen required to oxidize all organic material into carbon dioxide and water.
What are the 3 types of sewage treatment?
There are three main stages of the wastewater treatment process, aptly known as primary, secondary and tertiary water treatment.
What do cholesterol esters do?
Cholesterol esters are formed by acyl coenzyme A:cholesterol acyltransferase (ACAT) enzymes that play a key regulatory role in intestinal cholesterol absorption and provide core lipid for packaging of chylomicrons and hepatic-derived lipoproteins.
What is the difference between cholesterol and cholesteryl esters?
Cholesterol is an important sterol component in animals. The key difference between cholesterol and cholesteryl esters is the active and the inactive forms. Cholesterol is an active sterol form whereas cholesteryl ester is an inactive esterified form in which cholesterol is transported in the circulatory system.
What is the role of cholesteryl ester transfer protein?
Cholesteryl ester transfer protein (CETP), also called plasma lipid transfer protein, is a plasma protein that facilitates the transport of cholesteryl esters and triglycerides between the lipoproteins.
Are there any CETP inhibitors in the market?
Two potent CETP inhibitors (Anacetrapib and TA8995) are still in clinical development. Both are associated with a marked increase in HDLc levels and reduction in LDL-C level.
What kind of drug inhibits CETP transfer protein?
A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein (CETP).
How are CETP inhibitors used to treat atherosclerosis?
CETP Inhibitors. CETP is responsible for transferring cholesteryl esters from HDL to LDL or VLDL particles in exchange for TGs. Inhibition of CETP in an animal model reduced progression of atherosclerosis [73].
What’s the difference between HDL and CETP inhibition?
Inhibition of CETP was first recognized as a therapeutic target when individuals with homozygous deficiency (i.e. no CETP activity) were found to have mean HDL levels of approximately 160mg/dL and mean LDL levels of approximately 80mg/dl. Individuals with heterozygous deficiency had moderately elevated HDL without any difference in LDL.