The ATP-binding cassette A1 (ABCA1) transporter plays a major role in the efflux of lipids by mediating the
cellular transport of phospholipids and cholesterol to lipid-poor/lipid-free apolipoprotein A-I (apoA-I) particles and
thereby exerting important anti-atherogenic effects. Although the mechanism whereby ABCA1 mediates cholesterol efflux
is not completely understood, numerous studies have shown that, in addition to apoA-I, the expression level of the total
or cell surface ABCA1 protein is a determining factor for the activity of ABCA1-mediated cholesterol efflux, and defects
in ABCA1-mediated cholesterol efflux lead to various pathological conditions in different cells, including cardiovascular
and metabolic disorders. It has been widely demonstrated that a growing list of natural and synthetic substances and
metabolic regulators that modulate the expression of ABCA1 not only act directly on the ABCA1 gene promoter, but also
occurs at the post-transcriptional level via micro-RNAs and post-translationally through the stabilization or localization of
the protein. The complex regulatory network of ABCA1 results in promoting or suppressing cholesterol efflux from cells,
therefore we speculate that the ABCA1 transporter is emerging as a novel therapeutic target for cardiovascular and metabolic
disorders. Thus, ABCA1 is a key modulator of cellular cholesterol efflux and contributes to functional disorders in
different types of cells.
ABCA1, Cholesterol efflux, Atherosclerosis, HDL.
Department of Cardiology, Sun Yat-sen Memorial Hospital, University of Sun Yat-sen, Guangzhou, China.