Ezetimibe blocks internalization of the NPC1L1/cholesterol complex.
Niemann-Pick C1-like 1 (NPC1L1) is a target for ezetimibe, a drug that blocks intestinal cholesterol absorption. A new study by Ge et al. (2008) in this issue of Cell Metabolism shows that non-lipoprotein-bound cholesterol induces endocytosis of NPC1L1 and that ezetimibe blocks the internalization of the NPC1L1/cholesterol complex. The in vivo significance of these findings is discussed.
Chang
Ta-Yuan
TY
Department of Biochemistry, Dartmouth Medical School, Hanover, NH 03755, USA. ta.yuan.chang@dartmouth.edu
Chang
Catherine
C
D001384:Azetidines / Q000494:pharmacology*; D002784:Cholesterol / Q000378:metabolism* / Q000502:physiology; D004705:Endocytosis / Q000187:drug effects*; D000069438:Ezetimibe; D006801:Humans; D007408:Intestinal Absorption; D008565:Membrane Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism*; D026901:Membrane Transport Proteins
D001384:Azetidines; D008565:Membrane Proteins; D026901:Membrane Transport Proteins; C410800:NPC1L1 protein, human; D002784:Cholesterol; D000069438:Ezetimibe