Target intelligence / Profile preview

Oxidized apolipoprotein B-100 (oxApoB-100)

Target
oxApoB-100
Molecular classification
Apolipoprotein, Modified protein, Lipoprotein component, Scavenger receptor ligand
01

Overview

Oxidized apolipoprotein B-100 is a modified form of the structural protein found in low-density lipoprotein (LDL) particles, occurring primarily through oxidative stress in the arterial subendothelial space (Witztum & Steinberg, 1991). While native apolipoprotein B-100 is essential for cholesterol transport via the LDL receptor, its oxidized counterpart is recognized by scavenger receptors on macrophages, such as CD36 and LOX-1 (Gleissner et al., 2007). This unregulated uptake leads to the accumulation of cholesterol within macrophages, turning them into foam cells, which are central to the development and progression of atherosclerotic plaques (Lusis, 2000). Oxidized apolipoprotein B-100 also acts as a potent DAMP (damage-associated molecular pattern), triggering chronic inflammatory and immune responses within the vessel wall (Nilsson et al., 2012). Therapeutic strategies, including monoclonal antibodies like MLDL1278A and vaccines like CVX-210, aim to neutralize these oxidized epitopes to reduce vascular inflammation and the risk of acute cardiovascular events (Schiopu et al., 2004; Genentech, 2012). As a major driver of atherogenesis, it serves as both a critical biomarker for oxidative stress and a promising target for immunomodulatory cardiovascular therapies (Ylä-Herttuala et al., 2012).

Other names
Oxidized ApoB-100Malondialdehyde-modified apolipoprotein B-100MDA-ApoB-100Oxidized LDL-ApoBoxLDL-ApoB100Apolipoprotein B-100, oxidized
02

Mechanism of action

Monoclonal antibodies and vaccines target oxidized apolipoprotein B-100 to neutralize its pro-inflammatory epitopes and block its uptake by macrophage scavenger receptors, thereby preventing foam cell formation and stabilizing atherosclerotic plaques (Schiopu et al., 2004; Nilsson et al., 2012).

03

Biological functions

Lipid transportMacrophage activationPro-inflammatory signalingImmune response modulation
04

Disease associations

AtherosclerosisCardiovascular diseaseCoronary artery diseaseMyocardial infarctionStroke
05

Safety considerations

Immunogenicity of peptide-based vaccinesPotential for off-target systemic immune activationMaintaining specificity to avoid cross-reactivity with native ApoB-100Therapeutic challenges in targeting transiently modified epitopes in vivo
06

Interacting drugs

MLDL1278A

3 more in the full profile.

07

Biomarkers

Plasma oxidized LDL (oxLDL)Anti-oxApoB-100 autoantibodiesoxLDL/ApoB-100 ratioMalondialdehyde-modified LDL (MDA-LDL) levels

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