Cholesteryl ester (CE)

Cholesteryl esters (CEs) are highly hydrophobic lipid molecules formed by the esterification of cholesterol with fatty acids. They represent the primary storage form of cholesterol within cellular lipid droplets and serve as the main cargo in the hydrophobic core of circulating lipoproteins, such as low-density lipoprotein (LDL) and high-density lipoprotein (HDL). CEs are essential for systemic cholesterol homeostasis, facilitating the transport of cholesterol from peripheral tissues to the liver for excretion or recycling. Pathologically, the excessive accumulation of cholesteryl esters in arterial wall macrophages, leading to foam cell formation, is a hallmark of atherosclerosis and cardiovascular disease. While CEs are metabolites and not therapeutic protein targets themselves, they are central to the pharmacology of lipid-lowering therapies that target the enzymes and transporters regulating their levels. For instance, Cholesteryl Ester Transfer Protein (CETP) inhibitors aim to modulate CE transport to raise HDL-C, while Lysosomal Acid Lipase (LAL) replacement therapy is used to treat rare genetic storage disorders where CEs cannot be broken down.

Other names

Cholesterol esterSterol esterSteryl esterFatty acid ester of cholesterolCE

Pharmacological strategies modulate cholesteryl ester levels by inhibiting synthesis via Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors, inhibiting inter-lipoprotein transport via Cholesteryl Ester Transfer Protein (CETP) inhibitors, or replacing the deficient hydrolyzing enzyme through Lysosomal Acid Lipase (LAL) replacement therapy.