ATP-binding cassette transporter A1(ABCA1) is a kind of membrane intergrate protein and may have multiple and diverse functions. It mediates the cellular efflux of phospholipids and cholesterol to lipid-poor apolipoproteinA-Ⅰ(apoA-Ⅰ) and plays a significant role in high density lipoprotein (HDL) metabolism. Mutations in human ABCA1 cause severe HDL deficiencies characterized by the virtual absence of apoA-Ⅰ and HDL and prevalent atherosclerosis. ABCA1 expression is highly regulated and implies a variety of molecular actors. All of the nuclear receptors which involve in regulation of ABCA1 expression act via the DR4 element in the ABCA1 promoter. cAMP up-regulates ABCA1 expression by acting both at the transcriptional and translational level. Cytokines have been shown to exert pleiotropic and antinomic effects on ABCA1 transcription. In addition to these, some of enzymes and proteins such as protein kinase A, protein kinase CK2, cathepsin D are involved in the regulation of ABCA1 expression. The recent progress in the structure, function and regulation of ABCA1 transporter is reviewed.