ABCA1: an ATP-binding cassette (ABC) transporter that regulates cholesterol homeostasis and insulin secretion in beta-cells, and protects against cardiovascular disease. Inactivation of ABCA1 in beta-cells markedly impairs glucose tolerance and insulin secretion in mice. Rosiglitazone, an activator of the peroxisome proliferator-activated receptor-gamma, upregulates ABCA1 in beta-cells. ABCA1 expression in beta-cells is required for the beneficial effects of rosiglitazone on glucose tolerance. Mediates the transport of cholesterol and phospholipids from cells to HDL apolipoproteins, modulating HDL levels and atherogenesis. Induced by bacterial lipopolysaccharides (LPS) and repressed by ZNF202. Phosphorylation on Ser-2054 regulates phospholipid efflux. Unsaturated fatty acids destabilize ABCA1 by activating a PKC-delta pathway that phosphorylates ABCA1 serines. Defects in ABCA1 are a cause of high density lipoprotein deficiencies.
Protein type: Transporter; Membrane protein, integral; Vesicle; Transporter, ABC family; Membrane protein, multi-pass
Chromosomal Location of Human Ortholog: 9q31.1
Cellular Component: Golgi apparatus; perinuclear region of cytoplasm; integral to plasma membrane; endocytic vesicle; plasma membrane; phagocytic vesicle; lipid raft; external side of plasma membrane
Molecular Function: apolipoprotein A-I receptor activity; ATPase activity; cholesterol binding; apolipoprotein binding; ATPase binding; small GTPase binding; apolipoprotein A-I binding; protein binding; phospholipid transporter activity; syntaxin binding; cholesterol transporter activity; anion transmembrane transporter activity; phospholipid binding; ATP binding; receptor binding
Biological Process: response to drug; cholesterol metabolic process; regulation of Cdc42 protein signal transduction; intracellular cholesterol transport; cholesterol efflux; lipoprotein metabolic process; cellular lipid metabolic process; endosome transport; phospholipid translocation; G-protein coupled receptor protein signaling pathway; cholesterol homeostasis; reverse cholesterol transport; platelet dense granule organization and biogenesis; phospholipid efflux; lysosome organization and biogenesis; response to low density lipoprotein stimulus; positive regulation of cAMP biosynthetic process; protein amino acid lipidation; interleukin-1 beta secretion; phagocytosis, engulfment; response to nutrient; phospholipid homeostasis; peptide secretion
Disease: Hypoalphalipoproteinemia, Primary; Tangier Disease; Hypercholesterolemia, Familial
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