NPC1L1: Evolution From Pharmacological Target to Physiological Sterol Transporter [PDF]
Arteriosclerosis, Thrombosis, and Vascular Biology, 2006 Niemann-Pick C1-like 1 protein (NPC1L1) was recently shown to be the molecular target of the cholesterol absorption inhibitor class of drugs, of which ezetimibe is the first widely used member. Since its discovery, NPC1L1 has also been shown to play a focal physiological role in intestinal absorption of sterols, including plant sterols and cholesterol.
Murray W. Huff +2 more
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NPC1L1 knockout protects against colitis-associated tumorigenesis in mice [PDF]
BMC Cancer, 2015 Colorectal cancer is strongly associated with lipid metabolism. NPC1L1, a sterol transporter, plays a key role in modulating lipid homeostasis in vivo. Its inhibitor, ezetimibe, began to be used clinically to lower cholesterol and this caused the great debate on its role in causing carcinogenesis.
Jianming He +5 more
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Intestinal IL-25 prevents high-fat diet-induced obesity by modulating the cholesterol transporter NPC1L1 expression in the intestinal epithelial cells. [PDF]
Sci RepJeerawattanawart S, Angkasekwinai P.
europepmc +3 more sources
Ultrasound-Triggered NPC1L1-Targeting Nanobubbles for Remodeling the Tumor Microenvironment in Pancreatic Cancer Chemoimmunotherapy. [PDF]
ACS Appl Mater InterfacesDong L +6 more
europepmc +2 more sources
Niemann-Pick C1-Like 1 (NPC1L1) Inhibition and Cardiovascular Diseases [PDF]
Current Medicinal Chemistry, 2016 Circulating levels of cholesterol are derived from either endogenous production or intestinal absorption of dietary and biliary cholesterol. Niemann-Pick C1-Like 1 (NPC1L1) is a transmembrane protein that plays a key role in the intestinal absorption of cholesterol by facilitating its uptake through vesicular endocytosis. NPC1L1 is the molecular target
Angela Pirillo +2 more
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NPC1L1 and cholesterol transport [PDF]
FEBS Letters, 2010 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 ...
Betters, Jenna L., Yu, Liqing
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In Silico Analysis of the NPC1L1 Inhibitor of Catechins from Green Tea
Jurnal Info Kesehatan, 2023 The main contributor to cardiovascular disease is atherosclerosis. The Liver X Receptor is one of the unexplored signaling pathways in atherosclerosis that contributes to cholesterol efflux and inhibitory inflammation (LXR).
Erna Susanti, Ellyvına Setyadini
doaj +1 more source
The structure of the NPC1L1 N-terminal domain in a closed conformation. [PDF]
PLoS ONE, 2011 NPC1L1 is the molecular target of the cholesterol lowering drug Ezetimibe and mediates the intestinal absorption of cholesterol. Inhibition or deletion of NPC1L1 reduces intestinal cholesterol absorption, resulting in reduction of plasma cholesterol ...
Hyock Joo Kwon +2 more
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Ezetimibe Blocks Internalization of the NPC1L1/Cholesterol Complex [PDF]
Cell Metabolism, 2008 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.
Chang, Ta-Yuan, Chang, Catherine
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Journal of Lipid Research, 2008 Niemann-Pick C1-like 1 (NPC1L1) is a recently identified protein that mediates intestinal cholesterol absorption and regulates biliary cholesterol excretion. The itineraries and kinetics of NPC1L1 trafficking remain uncertain.
Nicole Hartwig Petersen +3 more
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