Document Detail


NPC1L1 and cholesterol transport.
MedLine Citation:
PMID:  20307540     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Jenna L Betters; Liqing Yu
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review     Date:  2010-03-19
Journal Detail:
Title:  FEBS letters     Volume:  584     ISSN:  1873-3468     ISO Abbreviation:  FEBS Lett.     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-06-14     Completed Date:  2010-07-05     Revised Date:  2012-01-31    
Medline Journal Info:
Nlm Unique ID:  0155157     Medline TA:  FEBS Lett     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  2740-7     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
Affiliation:
Department of Pathology Section on Lipid Sciences, Wake Forest University School of Medicine, Winston-Salem, NC 27157-1040, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Azetidines / pharmacology
Biological Transport / drug effects,  physiology*
Cholesterol / metabolism*
Humans
Membrane Proteins / genetics,  metabolism
Membrane Transport Proteins / drug effects,  genetics,  metabolism*
Substrate Specificity
Grant Support
ID/Acronym/Agency:
1F32DK084582-01/DK/NIDDK NIH HHS; R01 DK085176-01/DK/NIDDK NIH HHS
Chemical
Reg. No./Substance:
0/Azetidines; 0/Membrane Proteins; 0/Membrane Transport Proteins; 0/NPC1L1 protein, human; 0/Npc1l1 protein, mouse; 163222-33-1/ezetimibe; 57-88-5/Cholesterol
Comments/Corrections

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