Ezetimibe, a selective inhibitor of the transport of cholesterol.
Niemann-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.
Miura
Shin-ichiro
S
Department of Cardiology, Fukuoka University School of Medicine, Fukuoka, Japan.
Saku
Keijiro
K
D000818:Animals; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D001384:Azetidines / Q000494:pharmacology*; D002784:Cholesterol / Q000378:metabolism; D002986:Clinical Trials as Topic; D004359:Drug Therapy, Combination; D000069438:Ezetimibe; D006801:Humans; D006937:Hypercholesterolemia / Q000188:drug therapy / Q000378:metabolism; D008565:Membrane Proteins / Q000187:drug effects* / Q000378:metabolism; D026901:Membrane Transport Proteins; D051379:Mice; D017433:Protein Structure, Secondary
D000924:Anticholesteremic Agents; D001384:Azetidines; D008565:Membrane Proteins; D026901:Membrane Transport Proteins; C410800:NPC1L1 protein, human; D002784:Cholesterol; D000069438:Ezetimibe