High-density lipoprotein particle surface (HDL surface)

High-density lipoprotein (HDL) particle surfaces are dynamic molecular assemblies composed of a phospholipid monolayer, free cholesterol, and specialized proteins known as apolipoproteins, with Apolipoprotein A-I (ApoA-I) being the most prominent (Phillips, 2014, Journal of Lipid Research). These surfaces act as the functional interface for reverse cholesterol transport (RCT), a process where excess cholesterol is removed from peripheral tissues, such as arterial macrophages, and transported to the liver for biliary excretion (Zhu et al., 2020, Frontiers in Pharmacology). Beyond lipid homeostasis, the HDL surface serves as a platform for various enzymes, such as paraoxonase 1, that provide antioxidant and anti-inflammatory benefits, protecting the vascular endothelium (Rosenson et al., 2016, JACC). In drug development, HDL-like lipoprotein particle surfaces are targeted through the use of reconstituted HDL (rHDL) or HDL mimetics designed to rapidly enhance cholesterol efflux in patients with acute coronary syndrome or high-risk atherosclerosis (Gibson et al., 2016, Circulation). These therapeutic interventions, such as CSL112 and CER-001, aim to stabilize and reduce the volume of atherosclerotic plaques by mimicking the structural and functional properties of endogenous HDL particles (Tardif et al., 2014, European Heart Journal).

Other names

HDL-like lipoprotein particle surfacesHDL surfaceHigh-density lipoprotein surfaceReconstituted HDL surfaceHDL-like particles

Enhancement of cholesterol efflux from peripheral tissues (e.g., macrophages) via interaction with ABCA1 and ABCG1 transporters, followed by transport to the liver for excretion.