Target intelligence / Profile preview

Lecithin:cholesterol acyltransferase (LCAT)

Target
LCAT
Molecular classification
Enzyme, family of phospholipid:diacylglycerol acyltransferases
01

Overview

Lecithin:cholesterol acyltransferase (LCAT) is a soluble enzyme in the plasma that catalyzes the formation of cholesteryl esters from free cholesterol and phosphatidylcholine (lecithin), primarily on HDL particles. This conversion is essential for the maturation of HDL and the process of reverse cholesterol transport, carrying cholesterol from peripheral tissues back to the liver for removal. LCAT binds to both HDL and LDL, is activated by apolipoproteins (primarily ApoA-I), and has alpha- and beta-LCAT activities depending on the lipoprotein substrate. Genetic deficiency leads to rare diseases (familial LCAT deficiency and fish-eye disease) with renal and ocular manifestations, while altered LCAT activity is implicated in cardiovascular health and disease. The enzyme is a target for therapies aiming at enzyme replacement and modulation of cholesterol transport to treat related disorders

Other names
phosphatidylcholine-sterol O-acyltransferasephosphatidylcholine-sterol acyltransferasephospholipid-cholesterol acyltransferaseLCAT_HUMAN
02

Mechanism of action

Enzyme replacement (restores esterification in deficiency); Allosteric activation (gliflozins, sucrose, flavonoids increase LCAT activity); HDL-targeted therapies (potentially to enhance cholesterol efflux/HDL maturation)

03

Biological functions

Cholesterol esterificationReverse cholesterol transportHDL metabolismLipoprotein maturation
04

Disease associations

Familial LCAT deficiencyFish-eye diseaseCardiovascular disease / AtherosclerosisRenal disease (especially from LCAT deficiency)possibly other lipid metabolism disorders
05

Safety considerations

Renal impairment riskUncertain cardiovascular outcomeVisual impairment
06

Interacting drugs

Recombinant human LCAT

3 more in the full profile.

07

Biomarkers

LCAT activity in plasmaHDL cholesterol levelsCholesteryl ester percentage in plasmaother lipid panel measures in clinical enzymology

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