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.
journal_name
FEBS Lettjournal_title
FEBS lettersauthors
Betters JL,Yu Ldoi
10.1016/j.febslet.2010.03.030subject
Has Abstractpub_date
2010-07-02 00:00:00pages
2740-7issue
13eissn
0014-5793issn
1873-3468pii
S0014-5793(10)00242-5journal_volume
584pub_type
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