What are lipoproteins metabolised by?
What are lipoproteins metabolised by?
As the liver senses a decrease in cholesterol production, it attempts to compensate by increasing the number of LDL receptors on the surface of its cells, which leads to increased uptake of two lipoproteins, LDL and VLDL, into the liver, which then metabolizes into cholesterol and other molecules.
Do basic drugs bind to albumin?
Basic drugs associate with a number of plasma constituents. alpha 1-Acid glycoprotein, lipoprotein, and albumin all appear to play an important role in the binding of most of these drugs.
How is LDL metabolized?
LDL particles contain a core of cholesterol esters and a smaller amount of triglyceride. LDL is internalized by hepatic and nonhepatic tissues. In the liver, LDL is converted into bile acids and secreted into the intestines. In non hepatic tissues, LDL is used in hormone production, cell membrane synthesis, or stored.
What enzymes are involved in lipoprotein metabolism?
There are several enzymes and transfer proteins that play a key role in lipoprotein metabolism.
- Lipoprotein Lipase (LPL) (19)
- Hepatic Lipase (20)
- Endothelial Lipase (21)
- Lecithin: Cholesterol Acyltransferase (LCAT) (22)
- Cholesteryl Ester Transfer Protein (CETP) (23)
What drugs bind to albumin?
Albumin has hydrophobic binding domains in which drugs such as warfarin and diazepam can bind. Abraxane® is an established albumin-based nanoparticle system produced by Celgene and is used in the treatment of cancer.
Does warfarin bind to albumin?
Warfarin is a narrow therapeutic range drug and can cause major or fatal bleeding. Approximately 99% of the drug is bound to human plasma albumins [3]. One of the pharmacokinetic mechanisms for drug interactions with warfarin is protein binding interaction.
Do lipid soluble drugs bind to plasma proteins?
Plasma Protein Binding It is the non-ionized lipid-soluble form of the drug that is free to act, and it is unbound drug, i.e., drug that’s not bound to plasma proteins, that is also free to diffuse through membranes and act.
Why are lipoproteins needed to transport lipids in the bloodstream?
Lipoproteins Transport Lipids Around the Body. Lipoproteins are transport vehicles for moving water-insoluble lipids around the body. The interior of a lipoprotein—called the lipid core—carries the triglycerides and cholesterol esters, both of which are insoluble in water.
What drugs bind to lipoproteins?
Examples of drugs with high log P values that are known to bind to lipoproteins include cyclosporine A, amiodarone, halofantrine, amphotericin B, nystatin and eritoran. In evaluating the effects of increased plasma lipid content on the pharmacokinetics of drugs, it is important to consider the nature of the cause of the increased lipid levels.
What is the role of apolipoproteins in lipid metabolism?
The apolipoproteins are particularly important, as they play a role in classifying the lipoprotein into one of five main classes: chylomicrons, very-low-density lipoprotein (VLDL), intermediate-density lipoprotein (IDL), low-density lipoprotein (LDL), and high-density lipoprotein (HDL) provide structure and function in lipid metabolism.
Are plasma lipoproteins important in drug discovery and development?
The association of potential new drug candidates with plasma lipoproteins is often overlooked in drug discovery and development programmes. For many hydrophobic drugs, the level of free drug in the plasma might not always be associated with predictable outcomes of pharmacological activity.
What are the potential consequences of impaired lipoprotein metabolism?
An impairment in lipoprotein metabolism could lead to catastrophic implications in an affected individual. A pathologic increase in LDL, for example, is a known risk factor in cardiovascular disease as it leads to premature atherosclerotic changes of vessels.
