Target intelligence / Profile preview

Lysophosphatidylcholine acyltransferase 3 (LPCAT3)

Target
LPCAT3
Molecular classification
Enzyme, Membrane-bound O-acyltransferase (MBOAT) family, Acyltransferase
01

Overview

Lysophosphatidylcholine acyltransferase 3 (LPCAT3) is an integral membrane enzyme of the endoplasmic reticulum, belonging to the membrane-bound O-acyltransferase (MBOAT) family[1][3]. It catalyzes the reacylation of lysophosphatidylcholine (LPC) (and other lysophospholipids such as lyso-PE and lyso-PS) by preferentially incorporating polyunsaturated fatty acids, most notably arachidonic acid, into the sn-2 position of membrane phospholipids, notably phosphatidylcholine (PC)[2][3]. LPCAT3 is highly expressed in the liver, intestine, and adipose tissue—key organs for systemic lipid metabolism and lipoprotein production[1][4]. It is essential for maintaining the fluidity and structural properties of cellular membranes, regulation of triglyceride and lipoprotein secretion, and modulation of metabolic and inflammatory pathways[1][2][3][4]. Genetic and biochemical studies indicate that LPCAT3 activity affects circulating atherogenic lipoproteins, insulin sensitivity, and tissue-specific lipid composition. Dysregulation of LPCAT3 has been linked to metabolic, cardiovascular, and neurological diseases[1][4][5].

Other names
MBOAT5OACT5Lyso-PC acyltransferase 3LPLAT5LPLAT12O-acyltransferase domain-containing protein 5Lysophospholipid acyltransferase 5Lyso-PS acyltransferasenessy1-acylglycerophosphocholine O-acyltransferase1-acylglycerophosphoethanolamine O-acyltransferase1-acylglycerophosphoserine O-acyltransferaseC3F
02

Mechanism of action

Modulators are believed to regulate levels or activity of LPCAT3, influencing incorporation of polyunsaturated fatty acids (PUFAs), especially arachidonic acid, into membrane phospholipids and affecting downstream lipid signaling, lipoprotein assembly, and metabolic pathways[1][2][3][5].

03

Biological functions

Phospholipid remodelingRegulation of membrane fluidityLipid metabolismLipoprotein production and secretionRegulation of lipid absorptionRegulation of membrane composition and structureRegulation of cell proliferation
04

Disease associations

Cardiovascular disease (impact on lipoprotein metabolism, atherosclerosis)Metabolic disease (insulin resistance, lipid metabolism disorders)Neurological disease (regulation of bioactive lipids in neuropathology)Inflammation
05

Safety considerations

Modulating LPCAT3 may disrupt essential membrane phospholipid composition, with risks of impaired lipoprotein assembly, altered metabolic homeostasis, and possible unintended effects on cell membrane integrity and function[1][4].
06

Interacting drugs

No specific approved drugs directly targeting LPCAT3 identified in current search; inhibitors/modulators are under investigation in lipid metabolism and metabolic disease contexts[1][5].
07

Biomarkers

LPCAT3 expression/activity levels could serve as biomarkers for lipid metabolic status, risk of atherosclerosis, and possibly insulin sensitivity/resistance, but no clinically validated biomarker currently established[1][4][5].

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