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: Membrane protein, integral; Vesicle; Transporter; Membrane protein, multi-pass; Transporter, ABC family
Chromosomal Location of Human Ortholog: 9q31.1
Cellular Component: Golgi apparatus; integral to plasma membrane; perinuclear region of cytoplasm; endocytic vesicle; plasma membrane; phagocytic vesicle; external side of plasma membrane; lipid raft
Molecular Function: apolipoprotein A-I receptor activity; ATPase activity; cholesterol binding; apolipoprotein binding; ATPase binding; apolipoprotein A-I binding; small GTPase binding; protein binding; syntaxin binding; phospholipid transporter activity; cholesterol transporter activity; phospholipid binding; anion transmembrane transporter activity; ATP binding; receptor binding
Biological Process: response to drug; cholesterol metabolic process; regulation of Cdc42 protein signal transduction; lipoprotein metabolic process; intracellular cholesterol transport; cholesterol efflux; cellular lipid metabolic process; endosome transport; phospholipid translocation; G-protein coupled receptor protein signaling pathway; cholesterol homeostasis; reverse cholesterol transport; phospholipid efflux; platelet dense granule organization and biogenesis; 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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