Target intelligence / Profile preview

Oxidized low-density lipoprotein receptor 1 (LOX-1)

Target
LOX-1
Molecular classification
Receptor, Scavenger receptor, C-type lectin-like protein, Transmembrane protein
01

Overview

Oxidized low-density lipoprotein receptor 1 (LOX-1) is a type II membrane protein, encoded by the OLR1 gene, and is the principal receptor for oxidized LDL (oxLDL) in endothelial cells, macrophages, smooth muscle cells, and several other cell types[1][4][8]. LOX-1 belongs to the C-type lectin-like superfamily and mediates the binding, internalization, and degradation of oxLDL, contributing to the formation of foam cells and vascular dysfunction in atherosclerosis[1][3]. Its expression is highly inducible by atherogenic stimuli (e.g., inflammatory cytokines, hypertension, oxidized lipids, diabetes) and is low under physiological conditions[1][3][5]. LOX-1 also binds other ligands, including apoptotic cells, platelets, advanced glycation end-products, and bacteria[4]. Activation of LOX-1 by oxLDL initiates inflammatory, pro-adhesive, and apoptotic signaling pathways, making it a critical player in endothelial dysfunction and atherogenesis[1][3][4][5]. Soluble LOX-1 can be detected in the circulation and is investigated as a biomarker for cardiovascular disease risk[3]. Targeting LOX-1 is considered a promising therapeutic strategy for the prevention and treatment of cardiovascular and metabolic diseases associated with vascular injury[5].

Other names
Lectin-type oxidized LDL receptor 1OLR1Ox-LDL receptor 1
02

Mechanism of action

Inhibition or blockade of LOX-1 reduces oxLDL uptake and foam cell formation, attenuates vascular inflammation, and limits atherosclerotic progression[5]. Downregulation of LOX-1 expression can reduce endothelial dysfunction, apoptosis, and leukocyte adhesion[5][4].

03

Biological functions

Recognition and internalization of oxidized low-density lipoprotein (oxLDL)Endocytosis and degradation of oxLDLModulation of endothelial cell activation and dysfunctionLeukocyte adhesion and recruitmentRegulation of apoptosisInitiation of inflammatory signaling (e.g., NF-κB activation)Binding of apoptotic cells, activated platelets, and aged red blood cells
04

Disease associations

Cardiovascular disease (especially atherosclerosis)Acute myocardial infarctionVascular dysfunction and hypertensionDiabetes-related vascular complicationsPotential modifier in neurodegenerative disease (e.g., Alzheimer's disease)Inflammation
05

Safety considerations

Possible interference with physiological clearance of apoptotic cells and modified lipoproteins, which could have unwanted immunological effects[4]Modulation of LOX-1 may impact host defense mechanisms, given its role in innate immunity and scavenging function[4][5]Inhibition may affect vascular repair and remodeling via impaired recruitment of specific cell types[2][5]
06

Interacting drugs

No FDA-approved LOX-1–targeting therapeutics to date[3][5]

1 more in the full profile.

07

Biomarkers

Circulating soluble LOX-1 (sLOX-1) as a marker for endothelial dysfunction and cardiovascular risk[3]LOX-1 gene expression as a diagnostic or prognostic biomarker for atherosclerosis and myocardial infarction risk[3][5]

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