Apolipoprotein B-100 (ApoB-100) (ApoB-100)

Apolipoprotein B-100 (ApoB-100) is a large, 4536-amino acid protein that serves as the primary structural scaffold for atherogenic lipoproteins, including VLDL, IDL, and LDL (UniProt P04114). Synthesized in the liver, it is essential for the assembly and secretion of these particles and serves as the primary ligand for the LDL receptor (LDLR), mediating the endocytosis of LDL particles into cells (PubMed: 2515811). Elevated plasma concentrations of ApoB-100 are a major driver of atherosclerosis and are highly predictive of cardiovascular disease risk, as each atherogenic particle contains exactly one ApoB-100 molecule (StatPearls: Apolipoprotein B). Pharmacological targeting of ApoB-100 has been achieved through antisense oligonucleotides like mipomersen, which binds to ApoB mRNA to trigger its degradation and reduce protein synthesis (FDA: Kynamro Label). Additionally, microsomal triglyceride transfer protein (MTP) inhibitors like lomitapide indirectly target ApoB-100 by preventing its assembly into lipoproteins, though this is associated with risks of hepatic steatosis (PubMed: 23332144).

Other names

ApoBApolipoprotein BApo B-100Apolipoprotein B-100 precursor

Direct inhibition of protein synthesis via antisense oligonucleotides (e.g., mipomersen) that bind to ApoB-100 mRNA, leading to its degradation by RNase H. Indirect inhibition occurs via MTP inhibitors (e.g., lomitapide) which prevent the lipidation and assembly of ApoB-100 into VLDL particles.