FEBS Letters
Volume 584, Issue 13 , Pages 2740-2747, 2 July 2010

NPC1L1 and cholesterol transport

Edited by Wilhelm Just

Department of Pathology Section on Lipid Sciences, Wake Forest University School of Medicine, Winston-Salem, NC 27157-1040, USA

Received 19 February 2010; received in revised form 15 March 2010; accepted 16 March 2010. published online 22 March 2010.

Abstract 

The polytopic transmembrane protein, Niemann–Pick C1-Like 1 (NPC1L1), is enriched in the apical membrane of small intestine absorptive enterocytes where it mediates extracellular sterol transport across the brush border membrane. It is essential for intestinal sterol absorption and is the molecular target of ezetimibe, a potent cholesterol absorption inhibitor that lowers blood cholesterol in humans. NPC1L1 is also highly expressed in human liver. The hepatic function of NPC1L1 may be to limit excessive biliary cholesterol loss. NPC1L1-dependent sterol uptake seems to be a clathrin-mediated endocytic process and is regulated by cellular cholesterol content. Recently, NPC1L1 inhibition has been shown to have beneficial effects on components of the metabolic syndrome, such as obesity, insulin resistance, and fatty liver, in addition to atherosclerosis.

Keywords: Ezetimibe, Intestinal cholesterol absorption, Hypercholesterolemia, ABCG5/ABCG8

To access this article, please choose from the options below

Login to an existing account or Register a new account.

  • Purchase this article for 31.50 USD (You must login/register to purchase this article)

    Online access for 24 hours. The PDF version can be downloaded as your permanent record.

  • Subscribe to this title

    Get unlimited online access to this article and all other articles in this title 24/7 for one year.

  • Claim access now

    For current subscribers with Society Membership or Account Number.

  • Visit SciVerse ScienceDirect to see if you have access via your institution.
 

PII: S0014-5793(10)00242-5

doi:10.1016/j.febslet.2010.03.030

FEBS Letters
Volume 584, Issue 13 , Pages 2740-2747, 2 July 2010

Article Tools

* Image Usage & Resolution