Epidemiological studies have demonstrated that high density lipoprotein cholesterol (HDL-C) is inversely related to the incidence of coronary heart disease morbidity and mortality. In the present paper, we summarized the recently published data on HDL receptor, reverse cholesterol transport, and antiatherogenic effect of HDL particle. Several investigators have reported the apparent molecular weight of HDL binding protein using ligand blotting by radiolabeled HDL and immunoblotting by antibody against the purified binding protein. These results, however, were not consistent among the data reported from several laboratories. In 1992 a cDNA of HDL binding protein (HBP) was isolated from a human fibroblast and a human erythroleukemia cell cDNA library but it does not contain a classical hydrophobic membranes spanning domain. At present, it is reasonable to assume that HBP is different structurally and functionally from a classical plasma membrane receptor. We hope putative HDL receptor will be isolated, characterized and its cDNA will be cloned in the near future. It has been postulated that there are four functional steps in the pathway of reverse cholesterol transport. The main step is CETP-mediated transfer of cholesteryl esters from HDL to the VLDL/LDL fraction. Recent development of molecular biological techniques enable us to make a animal model over expressing apolipoprotein A-I or A-II, namely a transgenic mouse. These models indicated that apolipoprotein A-I has an antiatherogenic effect in vivo but apolipoprotein A-II does not.