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Ezetimibe, a selective inhibitor of the transport of cholesterol Miura S; Saku KIntern Med 2008[]; 47 (13): 1165-70Niemann-Pick C1-like 1 (NPC1L1) has recently been identified and has been shown to have features of a plasma membrane transporter, including a secretion signal, 13 predicted transmembrane domains, extensive N-linked glycosylation sites and a sterol-sensing domain. It is highly expressed on the surface of absorptive jejunal enterocytes. NPC1L1 has been shown to be a direct target of ezetimibe, and an ezetimibe-sensitive pathway plays a role in intestinal cholesterol absorption. Ezetimibe-based therapy represents an exciting new area in the treatment of dyslipidemia.|Animals[MESH]|Anticholesteremic Agents/*pharmacology[MESH]|Azetidines/*pharmacology[MESH]|Cholesterol/metabolism[MESH]|Clinical Trials as Topic[MESH]|Drug Therapy, Combination[MESH]|Ezetimibe[MESH]|Humans[MESH]|Hypercholesterolemia/drug therapy/metabolism[MESH]|Membrane Proteins/*drug effects/metabolism[MESH]|Membrane Transport Proteins[MESH]|Mice[MESH]|Protein Structure, Secondary[MESH] |
