The role of phospholipid transfer proteins (PLTPs) in atherogenesis goes beyond the transfer of phospholipids between lipoprotein particles. Genetic ablation of PLTPs in mice results in reduced hepatic secretion of apolipoprotein-B (apoB), the major protein of atherogenic lipoproteins. In this issue, Luo et al. interrogated the link between PLTP activity and apoB secretion in human hepatoma cells using a pharmacological screen to identify specific inhibitors of PLTPs. A series of 3-benzazepines demonstrated potent inhibition of PLTP activity and reduced apoB secretion from human hepatoma cells and primary mouse hepatocytes. These observations demonstrate that PLTPs regulate apoB secretion and that pharmacological inhibition of PLTP activity may provide a new avenue of therapeutic intervention for dyslipidemia.
See article at J Pharmacol Exp Ther 2010, 332:1100–1106.
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