Ezetimibe blocks internalization of the NPC1L1/cholesterol complex

Cell Metab. 2008 Jun;7(6):469-71. doi: 10.1016/j.cmet.2008.05.001.

Abstract

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.

Publication types

  • Review
  • Comment

MeSH terms

  • Azetidines / pharmacology*
  • Cholesterol / metabolism*
  • Cholesterol / physiology
  • Endocytosis / drug effects*
  • Ezetimibe
  • Humans
  • Intestinal Absorption
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / metabolism*
  • Membrane Transport Proteins

Substances

  • Azetidines
  • Membrane Proteins
  • Membrane Transport Proteins
  • NPC1L1 protein, human
  • Cholesterol
  • Ezetimibe