Cell membrane phospholipid interface

The cell membrane phospholipid interface and HDL-like phospholipid surfaces represent critical physicochemical environments that serve as therapeutic targets for various classes of drugs. In the context of infectious diseases, the bacterial cell membrane interface is targeted by lipopeptide and polymyxin antibiotics, which bind to and disrupt the lipid bilayer, leading to cell death (Source: NIH, PubMed). Conversely, in cardiovascular medicine, HDL-like phospholipid surfaces are utilized in the form of synthetic or recombinant high-density lipoprotein (HDL) mimetics, such as CER-001 or ETC-216, to facilitate reverse cholesterol transport (Source: Journal of the American College of Cardiology). These surfaces act as a scaffold for apolipoproteins and enzymes involved in lipid metabolism, promoting the efflux of cholesterol from atherosclerotic plaques. Therapeutic strategies targeting these interfaces rely on the amphipathic nature of drugs to interact with the hydrophobic and hydrophilic regions of the lipid bilayer. Consequently, these targets are pivotal for treating multi-drug resistant infections and managing dyslipidemia and atherosclerosis.

Other names

HDL-like phospholipid surfacesLipid bilayer interfacePhospholipid surfaceMembrane lipid interfaceHDL-mimetic surface

Drugs targeting these surfaces typically act by disrupting membrane integrity through pore formation and depolarization (in the case of lipopeptide antibiotics) or by acting as a physical sink to facilitate the efflux of cholesterol and other lipids from peripheral tissues (in the case of HDL mimetics).