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ATP-binding cassette sub-family A member 2 (ABCA2) is a membrane-bound transporter protein from the ABC superfamily, most highly expressed in neural tissues and macrophages. It is localized primarily to late endosomal/lysosomal membranes where it participates in the intracellular transport and homeostasis of cholesterol and sphingolipids—molecules critical for proper myelin formation and compaction in the nervous system. Expression of ABCA2 is associated with resistance to cancer drugs (especially those with steroid backbones) in several tumor models, and its genetic variants and regulation are implicated in pathologies such as Alzheimer’s disease, atherosclerosis, and cardiovascular disease. ABCA2 uses ATP hydrolysis to actively transport small hydrophobic molecules, contributing to homeostasis and potentially disease processes through effects on lipid metabolism and drug disposition.
Drug efflux by ATP-dependent active transport; Sequestration of cholesterol in late endosomal/lysosomal compartments; Modulation of cellular lipid environment affecting drug retention and resistance
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