Target intelligence / Profile preview

Lipoprotein-metabolism-related enzymes

Molecular classification
Enzyme, Hydrolase, Transferase
01

Overview

Lipoprotein-metabolism-related enzymes are a diverse group of proteins that regulate the composition and transport of lipids in the bloodstream. This class includes key enzymes such as lipoprotein lipase (LPL), which hydrolyzes triglycerides in VLDL and chylomicrons, and lecithin-cholesterol acyltransferase (LCAT), which esterifies cholesterol to facilitate HDL maturation (Feingold KR, Endotext, 2024). Other members, including hepatic lipase (HL) and endothelial lipase (EL), further modulate lipoprotein particles by acting on phospholipids and triglycerides (Santamarina-Fojo S, et al., J Biol Chem, 2004). Dysregulation of these enzymes is a central feature of dyslipidemia, contributing significantly to the development of atherosclerosis and coronary heart disease (Rader DJ, J Clin Invest, 2006). Therapeutic interventions often target these enzymes to improve lipid profiles; for example, fibrates increase LPL activity, while newer biologics like evinacumab inhibit ANGPTL3 to prevent the suppression of LPL and EL (Rosenson RS, et al., Nat Rev Cardiol, 2014).

Other names
Lipid metabolism enzymesLipoprotein lipases and acyltransferasesPlasma lipid-modifying enzymes
02

Mechanism of action

Modulation of triglyceride hydrolysis, cholesterol esterification, and lipid transfer between lipoprotein particles to optimize plasma lipid profiles (Feingold KR, Endotext, 2024; Rosenson RS, et al., Nat Rev Cardiol, 2014).

03

Biological functions

Lipid metabolismCholesterol esterificationTriglyceride hydrolysisLipoprotein remodeling
04

Disease associations

Cardiovascular diseaseDyslipidemiaAtherosclerosisHypertriglyceridemiaMetabolic syndrome
05

Safety considerations

HepatotoxicityMyopathyGastrointestinal side effectsIncreased risk of gallstonesOff-target cardiovascular effects (specific to some CETP inhibitors) (StatPearls, 2023; Rosenson RS, et al., Nat Rev Cardiol, 2014)
06

Interacting drugs

Fenofibrate

8 more in the full profile.

07

Biomarkers

Plasma triglyceridesLow-density lipoprotein cholesterol (LDL-C)High-density lipoprotein cholesterol (HDL-C)Apolipoprotein B (ApoB)Apolipoprotein A-I (ApoA-I)

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