Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as substrate. GSK264220A is a potent inhibitor of endothelial lipase (IC50 = 16 nM). Levels of HDL cholesterol are inversely correlated with endothelial lipase protein activity. Therefore, inhibition of endothelial lipase by compounds like GSK264220A may be expected to increase HDL levels and potentially decrease the risk of cardiovascular disease.
