Target intelligence / Profile preview

Phospholipid transfer protein (PLTP)

Target
PLTP
Molecular classification
Lipid transfer protein, Secreted plasma glycoprotein, BPI/LBP/CETP family (BPI fold-containing)
01

Overview

Phospholipid transfer protein (PLTP) is a secreted plasma glycoprotein involved in transferring phospholipids and other lipids, such as diacylglycerol and sphingomyelin, between lipoproteins’ surfaces, especially from triglyceride-rich lipoproteins to HDL[2][4]. It is critical in HDL particle remodeling and size regulation, impacting cholesterol metabolism and atherosclerosis risk. Structurally, PLTP belongs to the BPI/LBP/CETP protein family (BPI fold-containing), shares sequence similarity with cholesteryl ester transfer protein (CETP), and contains lipid-binding pockets necessary for lipid transfer activity[1][2]. Biologically, PLTP interacts with apolipoproteins (ApoA1, ApoA2) and lipoproteins (HDL, LDL, VLDL), forming complexes essential to its function. Elevated or altered PLTP activity has been associated with cardiovascular disease and metabolic disorders, making it a potential target, though with clinical implications that are still under active research[2][3].

Other names
BPIFELipid transfer protein IIBPI fold containing family EHDLCQ9phospholipid transfer proteinlipid transfer protein II
02

Mechanism of action

Drugs (in development) aim to modulate PLTP’s lipid transfer or remodeling activities to influence HDL cholesterol levels and lipoprotein particle profile[2].

03

Biological functions

Lipid and phospholipid transfer between lipoproteinsHigh-density lipoprotein (HDL) metabolismCholesterol metabolismRemodeling of HDL particle size and composition
04

Disease associations

Cardiovascular disease (HDL metabolism, atherosclerosis risk)DyslipidemiaOther (potentially involved in inflammation and metabolic syndrome)
05

Safety considerations

Targeting PLTP could have complex effects on lipoprotein metabolism, potentially impacting cholesterol transport and cardiovascular risk, with unknown long-term safetyalteration of HDL functionality may pose unforeseen risks[2]
06

Interacting drugs

None explicitly approved or established; no direct drug modulators are currently on the market or widely reported in literature as of 2024. Several research efforts are ongoing to develop PLTP inhibitors or modulators for atherosclerosis and dyslipidemia.
07

Biomarkers

Plasma PLTP activity or concentration has been studied as a biomarker for cardiovascular disease risk, HDL function, and efficacy of lipid-modifying therapies[2]

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