This article aims to highlight recent advanced knowledges in enzymes and transfer protein in lipoprotein metabolism, including lipoprotein lipase (LPL), hepatic triglyceride lipase (HTGL), lecithin: cholesterol acyltransferase (LCAT) and cholesteryl ester transfer protein (CETP). In addition to its traditional role in the hydrolysis of lipoproteins, recent studies have revealed other functions of LPL and HTGL which may serve as ligands of cell surface receptors and/or proteoglycans. Clinical studies also have demonstrated new aspects in genetic polymorphism of both enzymes related with coronary artery disease. Several animal models have provided exact functions of LCAT and CETP which play an important role of reverse cholesterol transport. Clinical approach of CETP deficiency may be useful to identify the mechanism of atherosclerosis.