Update on HDL receptors and cellular cholesterol transport.

Efflux is central to maintenance of tissue and whole body cholesterol homeostasis. The discovery of cell surface receptors that bind high-density lipoprotein (HDL) with high specificity and affinity to promote cholesterol release has significantly advanced our understanding of cholesterol efflux. We now know that 1) cells have several mechanisms to promote cholesterol release, including a passive mechanism that depends on the physico-chemical properties of cholesterol molecules and their interactions with phospholipids; 2) a variety of HDL particles can interact with receptors to promote cholesterol transport from tissues to the liver for excretion; and 3) interactions between HDL and receptors show functional synergy. Therefore, efflux efficiency depends both on the arrays of receptors on tissue cells and HDL particles in serum.