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, multi-pass; Transporter; Vesicle; Transporter, ABC family; Membrane protein, integral
Chromosomal Location of Human Ortholog: 9q31.1
Cellular Component: endocytic vesicle; external side of plasma membrane; Golgi apparatus; integral to plasma membrane; lipid raft; perinuclear region of cytoplasm; phagocytic vesicle; plasma membrane
Molecular Function: anion transmembrane transporter activity; apolipoprotein A-I binding; apolipoprotein A-I receptor activity; apolipoprotein binding; ATP binding; ATPase activity, coupled to transmembrane movement of substances; ATPase binding; cholesterol binding; cholesterol transporter activity; phospholipid binding; phospholipid transporter activity; protein binding; receptor binding; small GTPase binding; syntaxin binding
Biological Process: cellular lipid metabolic process; cholesterol efflux; cholesterol homeostasis; cholesterol metabolic process; endosome transport; G-protein coupled receptor protein signaling pathway; interleukin-1 beta secretion; intracellular cholesterol transport; lipoprotein metabolic process; lysosome organization and biogenesis; peptide secretion; phagocytosis, engulfment; phospholipid efflux; phospholipid homeostasis; phospholipid translocation; platelet dense granule organization and biogenesis; positive regulation of cAMP biosynthetic process; protein amino acid lipidation; regulation of Cdc42 protein signal transduction; response to drug; response to low density lipoprotein stimulus; response to nutrient; reverse cholesterol transport
Disease: Hypercholesterolemia, Familial; Hypoalphalipoproteinemia, Primary; Tangier Disease
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