Regulation of intestinal cholesterol absorption

David Q.H. Wang

Research output: Contribution to journalReview articlepeer-review

248 Scopus citations


The identification of defective structures in the ATP-binding cassette (ABC) transporters ABCG5 and ABCG8 in patients with sitosterolemia suggests that these two proteins are an apical sterol export pump promoting active efflux of cholesterol and plant sterols from enterocytes back into die intestinal lumen for excretion. The newly identified Niemann-Pick C1-like 1 (NPC1L1) protein is also expressed at the apical membrane of enterocytes and plays a crucial role in the ezetimibe-sensitive cholesterol absorption pathway. These findings indicate that cholesterol absorption is a multistep process that is regulated by multiple genes at the enterocyte level and that the efficiency of cholesterol absorption may be determined by the net effect between influx and efflux of intraluminal cholesterol molecules crossing the brush border membrane of the enterocyte. Combination therapy using cholesterol absorption (NPC1L1) inhibitor (ezetimibe) and 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase inhibitors (statins) provides a powerful novel strategy for the prevention and treatment of hypercholesterolemia.

Original languageEnglish (US)
Pages (from-to)221-248
Number of pages28
JournalAnnual review of physiology
StatePublished - 2007
Externally publishedYes


  • Bile salt
  • Chylomicron
  • Nutrition
  • Sitosterol
  • Transporter

ASJC Scopus subject areas

  • Physiology


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