The discovery of the role of the ATP-binding cassette transporter A1 (ABCA1) in mediating
apolipoprotein AI-mediated efflux has led to a dramatic increase in our knowledge of the
molecular mechanisms involved in cholesterol efflux and cellular metabolism. In this review,
we discuss several aspects of ABCA1 regulation including i) transcriptional regulation, ii)
substrate specificity and availability, iii) accessory proteins, iv) acceptor specificity and
availability, and v) protein trafficking. The majority of studies of ABCA1 regulation to date …