A low level of high-density lipoprotein (HDL) cholesterol is an important risk factor for coronary heart disease. Levels of HDL cholesterol and composition of HDL subclasses in plasma are regulated by many factors, including apolipoproteins, lipolytic enzymes, lipid transfer proteins, receptors, and cellular tansporters. Reverse transport of cholesterol from cells of the arterial wall to the liver is an important mechanism by which HDL exerts its anti-atherogenic properties. Enhancement of reverse cholesterol transport is considered as a potential target for anti-atherosclerotic drug therapy. It is suggested, however, that the serum level of HDL cholesterol does not necessarily reflect the efficacy of reverse cholesterol transport.