PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 22785139-2 2012 We used an atherosclerotic mouse model with histological features similar to those seen in ruptured human plaques to test the hypothesis that (1) dietary oxysterols accelerate plaque destabilization and rupture and (2) a NPC1L1 inhibitor, ezetimibe, has therapeutic effects on these processes. Ezetimibe 239-248 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 221-227 22007304-4 2012 Inhibition of cholesterol absorption with Ezetimibe, an inhibitor of Niemann Pick C1-like 1 (NPC1-L1), the major regulator of cholesterol absorption, increases cholesterol synthesis and hence the value of adding an inhibitor of cholesterol absorption to an inhibitor of cholesterol synthesis. Ezetimibe 42-51 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 69-91 22007304-4 2012 Inhibition of cholesterol absorption with Ezetimibe, an inhibitor of Niemann Pick C1-like 1 (NPC1-L1), the major regulator of cholesterol absorption, increases cholesterol synthesis and hence the value of adding an inhibitor of cholesterol absorption to an inhibitor of cholesterol synthesis. Ezetimibe 42-51 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 93-100 21683156-1 2011 Niemann-Pick C1-Like 1 (NPC1L1) is highly expressed in the small intestine across mammalian species and is the target of ezetimibe, a potent cholesterol absorption inhibitor. Ezetimibe 121-130 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-22 22579005-6 2012 Ezetimibe, a selective inhibitor of intestinal NPC1L1, is the widespread lipid-lowering agent. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 47-53 21683156-1 2011 Niemann-Pick C1-Like 1 (NPC1L1) is highly expressed in the small intestine across mammalian species and is the target of ezetimibe, a potent cholesterol absorption inhibitor. Ezetimibe 121-130 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 24-30 21437027-8 2011 On the other hand, common polymorphisms affecting the NPC1L1 transporter can interfere with the action of ezetimibe. Ezetimibe 106-115 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 54-60 20705552-5 2010 Recent studies show that genetic variation in Niemann-Pick C1-like 1 may be responsible for the inter-individual variability observed in the rates of intestinal cholesterol absorption and the response to ezetimibe. Ezetimibe 204-213 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 46-68 20953676-1 2011 PURPOSE: Niemann-Pick C1-like 1 (NPC1L1), a pharmacological target of ezetimibe, is responsible for cholesterol absorption in enterocytes and hepatocytes. Ezetimibe 70-79 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 9-31 20953676-1 2011 PURPOSE: Niemann-Pick C1-like 1 (NPC1L1), a pharmacological target of ezetimibe, is responsible for cholesterol absorption in enterocytes and hepatocytes. Ezetimibe 70-79 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 33-39 22358082-1 2011 Ezetimibe is the first agent used in hypercholesterolemia treatment known to lower intestinal cholesterol uptake that is able to inhibit NPC1L1 transport proteins in the brush boarder of enterocytes and macrophages. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 137-143 20809793-5 2011 NPC1L1 is the molecular target of ezetimibe, a potent cholesterol absorption inhibitor that is widely used in treating hypercholesterolemia. Ezetimibe 34-43 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-6 20699423-2 2010 Ezetimibe, by inhibiting NPC1L1 function, is widely used to treat hypercholesterolemia in humans. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 25-31 20543520-5 2010 Ezetimibe, an inhibitor of intestinal cholesterol absorption through its binding to Niemann-Pick C1-like 1 (NPC1L1), has been widely used for decreasing serum LDL-cholesterol levels in patients with hypercholesterolemia. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 84-106 20543520-5 2010 Ezetimibe, an inhibitor of intestinal cholesterol absorption through its binding to Niemann-Pick C1-like 1 (NPC1L1), has been widely used for decreasing serum LDL-cholesterol levels in patients with hypercholesterolemia. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 108-114 20601094-2 2010 Ezetimibe, an inhibitor of intestinal cholesterol absorption, inhibits Niemann-Pick C1-like 1 (NPC1L1). Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 71-93 20601094-2 2010 Ezetimibe, an inhibitor of intestinal cholesterol absorption, inhibits Niemann-Pick C1-like 1 (NPC1L1). Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 95-101 20403165-7 2010 We first incubated the cells with the micelles in the presence and absence of ezetimibe, the specific inhibitor of NPC1L1, to see whether the uptake of the cholesterol in the cells was mediated by NPC1L1. Ezetimibe 78-87 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 115-121 19907422-1 2010 The potent cholesterol absorption inhibitor ezetimibe was developed as a first-in-class drug for treating hypercholesterolemia even before its molecular target, Niemann-Pick C1-like 1 (NPC1L1), had been identified. Ezetimibe 44-53 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 161-183 20222991-0 2010 NPC1L1 inhibitor ezetimibe is a reliable therapeutic agent for non-obese patients with nonalcoholic fatty liver disease. Ezetimibe 17-26 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-6 19907422-1 2010 The potent cholesterol absorption inhibitor ezetimibe was developed as a first-in-class drug for treating hypercholesterolemia even before its molecular target, Niemann-Pick C1-like 1 (NPC1L1), had been identified. Ezetimibe 44-53 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 185-191 19631535-1 2009 During our effort to design a receptor binding assay to aid in the elucidation of the molecular mechanism of ezetimibe, we prepared a sulfur-35 containing radioligand which exhibits improved potency over the glucuronide conjugate of ezetimibe in both native enterocyte brush border membranes and membranes from cells expressing recombinant NPC1L1. Ezetimibe 233-242 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 340-346 19355905-7 2009 Recent studies from experimental animal models and preliminary findings in humans also suggest that blocking intestinal absorption of cholesterol with the powerful, specific, and effective NPC1L1 inhibitor ezetimibe, may offer a novel and exciting strategy for the treatment of cholesterol gallstones. Ezetimibe 206-215 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 189-195 19325169-3 2009 Ezetimibe, a clinically used cholesterol absorption inhibitor, blocks the endocytosis of NPC1L1 thereby inhibiting cholesterol uptake. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 89-95 19325169-9 2009 Ezetimibe-glucuronide, the major metabolite of ezetimibe in vivo, can block the internalization of NPC1L1 and cholesterol. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 99-105 19325169-9 2009 Ezetimibe-glucuronide, the major metabolite of ezetimibe in vivo, can block the internalization of NPC1L1 and cholesterol. Ezetimibe 47-56 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 99-105 19768174-9 2009 However, ezetimibe treatment of HepG2 (hepatocytes) and Caco-2 (enterocytes) cells caused a slight increase in PCSK9 and NPC1L1 mRNA, but no significant rise in PCSK9 protein secretion, suggesting that these transformed cells are not ideal model cell lines. Ezetimibe 9-18 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 121-127 18522832-7 2008 Together, our data suggest a model wherein cholesterol is internalized into cells with NPC1L1 through clathrin/AP2-mediated endocytosis and ezetimibe inhibits cholesterol absorption by blocking the internalization of NPC1L1. Ezetimibe 140-149 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 217-223 18403720-6 2008 Furthermore, using human NPC1L1 overexpression system, we demonstrated that both cholesterol and alpha-tocopherol uptake was also significantly increased by the overexpression of human NPC1L1 and ezetimibe inhibited their uptake. Ezetimibe 196-205 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 25-31 18403720-6 2008 Furthermore, using human NPC1L1 overexpression system, we demonstrated that both cholesterol and alpha-tocopherol uptake was also significantly increased by the overexpression of human NPC1L1 and ezetimibe inhibited their uptake. Ezetimibe 196-205 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 185-191 18522826-1 2008 Niemann-Pick C1-like 1 (NPC1L1) is a target for ezetimibe, a drug that blocks intestinal cholesterol absorption. Ezetimibe 48-57 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-22 18522826-1 2008 Niemann-Pick C1-like 1 (NPC1L1) is a target for ezetimibe, a drug that blocks intestinal cholesterol absorption. Ezetimibe 48-57 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 24-30 18522832-0 2008 The cholesterol absorption inhibitor ezetimibe acts by blocking the sterol-induced internalization of NPC1L1. Ezetimibe 37-46 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 102-108 18522832-2 2008 Ezetimibe, a hypocholesterolemic drug, has been reported to bind NPC1L1 and block cholesterol absorption. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 65-71 18460917-3 2008 In 2004, NPC1L1 was identified to be essential for intestinal cholesterol absorption, a process that is sensitive to a cholesterol absorption inhibitor ezetimibe. Ezetimibe 152-161 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 9-15 18551036-2 2008 Ezetimibe, an inhibitor of the intestinal cholesterol uptake protein Niemann-Pick C 1 like 1, is another drug for which genetic polymorphisms of hepatic organic anion transporting polypeptides (OATPs) are expected to be of clinical relevance because ezetimibe undergoes intensive enterohepatic circulation for which hepatic uptake transporters may be rate-limiting determinants. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 69-92 18551036-2 2008 Ezetimibe, an inhibitor of the intestinal cholesterol uptake protein Niemann-Pick C 1 like 1, is another drug for which genetic polymorphisms of hepatic organic anion transporting polypeptides (OATPs) are expected to be of clinical relevance because ezetimibe undergoes intensive enterohepatic circulation for which hepatic uptake transporters may be rate-limiting determinants. Ezetimibe 250-259 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 69-92 18227492-7 2008 An effective NPC1-L1 inhibitor (ezetimibe) improves the reduction in cholesterol caused by statins. Ezetimibe 32-41 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 13-20 18496605-7 2008 The discovery of the role of NPC1L1 in intestinal sterol transport occurred directly as a consequence of efforts to identify the molecular target of ezetimibe, a novel, potent, and specific inhibitor of sterol absorption that is now widely used in combination therapy with statins for the management of hypercholesterolemia in the general population. Ezetimibe 149-158 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 29-35 16177187-0 2005 Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. Ezetimibe 146-155 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 82-88 17880278-1 2007 NPC1L1 (Niemann-Pick C1-like 1), the pharmacological target of the cholesterol-uptake inhibitor ezetimibe, is a transporter localized on the brush border of enterocytes. Ezetimibe 96-105 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-6 17880278-1 2007 NPC1L1 (Niemann-Pick C1-like 1), the pharmacological target of the cholesterol-uptake inhibitor ezetimibe, is a transporter localized on the brush border of enterocytes. Ezetimibe 96-105 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 8-30 17662536-5 2007 The NPC1L1 gene has recently been identified as the target for the drug ezetimibe (Zetia), a cholesterol absorption inhibitor, and has been shown to be an intestinal cholesterol transporter. Ezetimibe 72-81 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 4-10 17662536-5 2007 The NPC1L1 gene has recently been identified as the target for the drug ezetimibe (Zetia), a cholesterol absorption inhibitor, and has been shown to be an intestinal cholesterol transporter. Ezetimibe 83-88 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 4-10 16513445-1 2006 BACKGROUND AND AIMS: Ezetimibe is an inhibitor of the cholesterol uptake transporter Niemann-Pick C1-like protein (NPC1L1). Ezetimibe 21-30 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 115-121 16297596-0 2005 Sequence variation in NPC1L1 and association with improved LDL-cholesterol lowering in response to ezetimibe treatment. Ezetimibe 99-108 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 22-28 16297596-3 2005 To test the hypothesis that genetic variation in NPC1L1 could influence the LDL-C response to ezetimibe, we performed extensive resequencing of the gene in 375 apparently healthy individuals and genotyped hypercholesterolemic patients from clinical trial cohorts. Ezetimibe 94-103 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 49-55 16297596-6 2005 Our data demonstrate that DNA sequence variants in NPC1L1 are associated with an improvement in response to ezetimibe pharmacotherapy and suggest that detailed analysis of genetic variability in clinical trial cohorts can lead to improved understanding of factors contributing to variable drug response. Ezetimibe 108-117 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 51-57 17140581-6 2007 The highest response to ezetimibe was observed in a carrier of R174H substitution in NPC1L1, which had been found to be associated with high cholesterol absorption. Ezetimibe 24-33 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 85-91 17473178-1 2007 Niemann-Pick C1-like 1 protein (NPC1L1) is the putative intestinal sterol transporter and the molecular target of ezetimibe, a potent inhibitor of cholesterol absorption. Ezetimibe 114-123 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-30 17473178-1 2007 Niemann-Pick C1-like 1 protein (NPC1L1) is the putative intestinal sterol transporter and the molecular target of ezetimibe, a potent inhibitor of cholesterol absorption. Ezetimibe 114-123 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 32-38 17571164-10 2007 These findings suggest that in humans, ezetimibe may reduce plasma cholesterol by inhibiting NPC1L1 function in both intestine and liver, and hepatic NPC1L1 may have evolved to protect the body from excessive biliary loss of cholesterol. Ezetimibe 39-48 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 93-99 17135346-7 2007 Furthermore, it was confirmed that sterol uptake increased by NPC1L1 overexpression was inhibited by ezetimibe. Ezetimibe 101-110 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 62-68 17002594-2 2007 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. Ezetimibe 149-158 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 21-43 17002594-2 2007 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. Ezetimibe 149-158 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 45-51 16407187-6 2006 This translocation was associated with a remarkable increase in cellular cholesterol uptake, which in turn was dose-dependently inhibited by ezetimibe, a novel cholesterol absorption inhibitor that specifically binds to NPC1L1. Ezetimibe 141-150 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 220-226 15679830-0 2005 Compound heterozygosity for two non-synonymous polymorphisms in NPC1L1 in a non-responder to ezetimibe. Ezetimibe 93-102 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 64-70 16098225-3 2005 We next hypothesized that common variants in NPC1L1 would underlie less extreme inter-individual variations in the plasma LDL cholesterol response to ezetimibe. Ezetimibe 150-159 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 45-51 16098225-4 2005 RESULTS: In 101 dyslipidemic subjects, we found that NPC1L1 haplotype was significantly associated with inter-individual variation in the response of plasma LDL cholesterol to treatment with ezetimibe for 12 weeks. Ezetimibe 191-200 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 53-59 16083725-8 2005 Combination therapy using a novel, specific, and potent cholesterol absorption (NPC1L1) inhibitor (ezetimibe) and HMG-CoA reductase inhibitors (statins) offers an efficacious new approach to the prevention and treatment of hypercholesterolemia. Ezetimibe 99-108 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 80-86 15928087-2 2005 Using a genetic approach, we recently identified Niemann-Pick C1-Like 1 (NPC1L1) as a critical mediator of cholesterol absorption and an essential component of the ezetimibe-sensitive pathway. Ezetimibe 164-173 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 49-71 15928087-2 2005 Using a genetic approach, we recently identified Niemann-Pick C1-Like 1 (NPC1L1) as a critical mediator of cholesterol absorption and an essential component of the ezetimibe-sensitive pathway. Ezetimibe 164-173 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 73-79 15928087-3 2005 To determine whether NPC1L1 is the direct molecular target of ezetimibe, we have developed a binding assay and shown that labeled ezetimibe glucuronide binds specifically to a single site in brush border membranes and to human embryonic kidney 293 cells expressing NPC1L1. Ezetimibe 62-71 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 21-27 15928087-4 2005 Moreover, the binding affinities of ezetimibe and several key analogs to recombinant NPC1L1 are virtually identical to those observed for native enterocyte membranes. Ezetimibe 36-45 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 85-91 15679830-2 2005 The NPC1L1 gene product was recently identified as the molecular target for ezetimibe, although functional details are incomplete. Ezetimibe 76-85 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 4-10 15679830-3 2005 We used the non-response phenotype of plasma LDL cholesterol to ezetimibe treatment to ascertain individuals who might have variant NPC1L1. Ezetimibe 64-73 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 132-138 15679830-4 2005 We found that one non-responder to ezetimibe was a compound heterozygote for two rare non-synonymous polymorphisms in NPC1L1 that were absent in normal control subjects. Ezetimibe 35-44 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 118-124 15679830-6 2005 While there are many explanations for non-response to medications, our data suggest a possible relationship between NPC1L1 variation and ezetimibe response and further indicate that a non-response phenotype might ascertain subjects with genomic DNA variants that could help define metabolic pathways. Ezetimibe 137-146 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 116-122 34067439-1 2021 Ezetimibe is a well-known drug that lowers blood cholesterol levels by reducing its absorption in the small intestine when joining to Niemann-Pick C1-like protein (NPC1L1). Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 164-170 34511128-3 2021 Niemann-Pick C1-Like 1 (NPC1L1), a target of ezetimibe, plays an essential role in the absorption of intestinal cholesterol. Ezetimibe 45-54 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 24-30 33760662-1 2021 Niemann-Pick C1 Like-1 (NPC1L1) mediates the uptake of micellar cholesterol by intestinal epithelial cells and is the molecular target of the cholesterol-lowering drug ezetimibe (EZE). Ezetimibe 168-177 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-22 33760662-1 2021 Niemann-Pick C1 Like-1 (NPC1L1) mediates the uptake of micellar cholesterol by intestinal epithelial cells and is the molecular target of the cholesterol-lowering drug ezetimibe (EZE). Ezetimibe 168-177 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 24-30 33760662-1 2021 Niemann-Pick C1 Like-1 (NPC1L1) mediates the uptake of micellar cholesterol by intestinal epithelial cells and is the molecular target of the cholesterol-lowering drug ezetimibe (EZE). Ezetimibe 179-182 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-22 33760662-1 2021 Niemann-Pick C1 Like-1 (NPC1L1) mediates the uptake of micellar cholesterol by intestinal epithelial cells and is the molecular target of the cholesterol-lowering drug ezetimibe (EZE). Ezetimibe 179-182 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 24-30 34407950-2 2021 The drug ezetimibe inhibits NPC1L1-mediated absorption of cholesterol, lowering of circulating levels of low-density lipoprotein cholesterol. Ezetimibe 9-18 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 28-34 34272236-1 2021 Niemann-Pick C1-like 1 (NPC1L1) protein plays a central role in the intestinal cholesterol absorption and is the target of a drug, ezetimibe, which inhibits NPC1L1 to reduce cholesterol absorption. Ezetimibe 131-140 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 24-30 34272236-1 2021 Niemann-Pick C1-like 1 (NPC1L1) protein plays a central role in the intestinal cholesterol absorption and is the target of a drug, ezetimibe, which inhibits NPC1L1 to reduce cholesterol absorption. Ezetimibe 131-140 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 157-163 34272236-2 2021 Here, we present cryo-electron microscopy structures of human NPC1L1 in apo state, cholesterol-enriched state, and ezetimibe-bound state to reveal molecular details of NPC1L1-mediated cholesterol uptake and ezetimibe inhibition. Ezetimibe 207-216 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 62-68 34272236-4 2021 Upon increasing cholesterol level, SSD binds more cholesterol molecules, which, in turn, triggers the formation of a stable structural cluster in SSD, while binding of ezetimibe causes the deformation of the SSD and destroys the structural cluster, leading to the inhibition of NPC1L1 function. Ezetimibe 168-177 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 278-284 34067439-6 2021 It also shows interesting results when it comes to a pharmacophore study based on ezetimibe as the main ligand in lowering blood cholesterol levels, revealing which substituents on the azetidine-2-one ring are more similar to the ezetimibe skeleton and will more likely bind to NPC1L1 than ezetimibe. Ezetimibe 82-91 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 278-284 32368969-6 2021 Ezetimibe inhibits cholesterol absorption by targeting the Niemann-Pick C1-like 1 protein (NPC1L1), which is related to cholesterol absorption in the intestines. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 59-89 35063734-4 2022 Ezetimibe is the first, and only, NPC1L1 inhibitor approved for the treatment of hypercholesterolemia through decreasing cholesterol absorption for nearly two decades. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 34-40 32853776-7 2021 Ezetimibe is known to inhibit cholesterol absorption by blocking the activity of Niemann-Pick C1 like 1 (NPC1L1) protein, and simvastatin is known to enhance NPC1L1 expression in the human body"s small intestine. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 81-103 32853776-7 2021 Ezetimibe is known to inhibit cholesterol absorption by blocking the activity of Niemann-Pick C1 like 1 (NPC1L1) protein, and simvastatin is known to enhance NPC1L1 expression in the human body"s small intestine. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 105-111 32368969-6 2021 Ezetimibe inhibits cholesterol absorption by targeting the Niemann-Pick C1-like 1 protein (NPC1L1), which is related to cholesterol absorption in the intestines. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 91-97 32596471-0 2020 Cryo-EM structures of NPC1L1 reveal mechanisms of cholesterol transport and ezetimibe inhibition. Ezetimibe 76-85 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 22-28 32860884-1 2020 Ezetimibe inhibits Niemann-Pick C1-like 1 (NPC1L1) protein, which mediates intracellular cholesterol trafficking from the brush border membrane to the endoplasmic reticulum, where chylomicron assembly takes place in enterocytes or in the intestinal absorptive epithelial cells. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 43-49 32860884-3 2020 The aim of this study was to examine the effect of ezetimibe, a potent NPC1L1 inhibitor, on trans-epithelial lipid transport, and chylomicron assembly and secretion in enterocytes. Ezetimibe 51-60 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 71-77 32596471-1 2020 The intestinal absorption of cholesterol is mediated by a multipass membrane protein, Niemann-Pick C1-Like 1 (NPC1L1), the molecular target of a cholesterol lowering therapy ezetimibe. Ezetimibe 174-183 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 86-108 32596471-1 2020 The intestinal absorption of cholesterol is mediated by a multipass membrane protein, Niemann-Pick C1-Like 1 (NPC1L1), the molecular target of a cholesterol lowering therapy ezetimibe. Ezetimibe 174-183 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 110-116 32596471-3 2020 Here, we present two cryo-electron microscopy structures of NPC1L1, one in its apo form and the other complexed with ezetimibe. Ezetimibe 117-126 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 60-66 30994973-1 2019 Ezetimibe (EZE) and glucuronidated EZE (EZE-Glu) differentially target Niemann-Pick C1-like 1 (NPC1L1) and CD13 (aminopeptidase-N) to inhibit intestinal cholesterol absorption and cholesterol processing in other cells, although the precise molecular mechanisms are not fully elucidated. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 71-93 32410728-5 2020 The widely prescribed cholesterol uptake inhibitor, ezetimibe, blocks NPC1L1; we show that residues that lie at the interface between NPC1L1"s three extracellular domains comprise the drug"s binding site. Ezetimibe 52-61 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 70-76 32410728-5 2020 The widely prescribed cholesterol uptake inhibitor, ezetimibe, blocks NPC1L1; we show that residues that lie at the interface between NPC1L1"s three extracellular domains comprise the drug"s binding site. Ezetimibe 52-61 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 134-140 32410728-6 2020 These data support a model in which cholesterol passes through the cores of NPC1/NPC1L1 proteins; concerted movement of various domains is needed for transfer and ezetimibe blocks transport by binding to multiple domains simultaneously. Ezetimibe 163-172 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 81-87 31682937-3 2020 However, short-term applications of ezetimibe, which inhibits Npc1l1, were not associated with reduced vitamin D uptake in animals and humans. Ezetimibe 36-45 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 62-68 31682937-4 2020 The current study aimed to elucidate the effect of long-term inhibition of Npc1l1 by ezetimibe on the uptake and storage of orally administered triple deuterated vitamin D3 (vitamin D3-d3). Ezetimibe 85-94 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 75-81 30994973-1 2019 Ezetimibe (EZE) and glucuronidated EZE (EZE-Glu) differentially target Niemann-Pick C1-like 1 (NPC1L1) and CD13 (aminopeptidase-N) to inhibit intestinal cholesterol absorption and cholesterol processing in other cells, although the precise molecular mechanisms are not fully elucidated. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 95-101 29106532-2 2017 We tested the hypothesis that genetic variation in NPC1L1, mimicking treatment with ezetimibe, was associated with an increased risk of cancer. Ezetimibe 84-93 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 51-57 31064810-10 2019 SIGNIFICANCE STATEMENT: Niemann-Pick C1-Like 1 (NPC1L1) protein, a cholesterol importer and a molecular target of ezetimibe clinically used for dyslipidemia, is highly expressed not only in the intestine, but also in the liver in humans, although the pathophysiological importance of hepatic NPC1L1 in atherosclerotic diseases remained unclear. Ezetimibe 114-123 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 48-54 31064810-10 2019 SIGNIFICANCE STATEMENT: Niemann-Pick C1-Like 1 (NPC1L1) protein, a cholesterol importer and a molecular target of ezetimibe clinically used for dyslipidemia, is highly expressed not only in the intestine, but also in the liver in humans, although the pathophysiological importance of hepatic NPC1L1 in atherosclerotic diseases remained unclear. Ezetimibe 114-123 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 292-298 30391500-3 2018 Ezetimibe is an FDA-approved drug that reduces cholesterol uptake by inhibiting the endocytosis through Niemman-Pick C1-Like 1 (NPC1L1) receptor, expressed on the membrane of enterocytes and hepatocytes. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 128-134 30391500-5 2018 Blockage of NPC1L1 with ezetimibe in concentrations up to 50 muM does not reduce cell viability but diminished total cellular cholesterol, the percentage of infected cells, viral yield, viral RNA and protein synthesis without affecting DENV binding and/or entry to Huh-7 cells. Ezetimibe 24-33 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 12-18 29106532-13 2017 Conclusions: Lifelong, genetic inhibition of NPC1L1, mimicking treatment with ezetimibe, does not associate with risk of cancer. Ezetimibe 78-87 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 45-51 28478831-6 2017 Just as this protein is key in the entero-hepatic cycle of cholesterol, we hypothesize that there is an entero-hepatic cycle of HCV that could be disrupted by blocking NPC1L1 with ezetimibe, an already approved and readily available safe drug. Ezetimibe 180-189 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 168-174 28315682-7 2017 In this study, we found that treatment of cells that stably express NPC1L1-GFP with alpha-tocopherol promotes NPC1L1 endocytosis, and the NPC1L1 inhibitor, ezetimibe, efficiently prevents the alpha-tocopherol-induced endocytosis of NPC1L1. Ezetimibe 156-165 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 68-74 28203044-5 2017 The patient was placed on a low cholesterol/low plant sterol diet and treated with colestimide (a bile acid sequestrant) and ezetimibe (an NPC1L1 inhibitor). Ezetimibe 125-134 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 139-145 28167864-3 2017 Ezetimibe, which inhibits cholesterol absorption by inhibition of Niemann-Pick C1 like 1 (NPC1L1) protein in the brush border of intestinal cells, has been suggested as a new therapeutic option in these patients. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 66-88 28167864-3 2017 Ezetimibe, which inhibits cholesterol absorption by inhibition of Niemann-Pick C1 like 1 (NPC1L1) protein in the brush border of intestinal cells, has been suggested as a new therapeutic option in these patients. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 90-96 28057006-5 2017 RESULTS: We found that confluent Caco-2 cells expressed NPC1L1, and the absorption of cholesterol in the cells was inhibited by ezetimibe, a specific inhibitor of NPC1L1. Ezetimibe 128-137 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 56-62 28057006-5 2017 RESULTS: We found that confluent Caco-2 cells expressed NPC1L1, and the absorption of cholesterol in the cells was inhibited by ezetimibe, a specific inhibitor of NPC1L1. Ezetimibe 128-137 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 163-169 27714510-6 2016 By potently inhibiting the Niemann-Pick C1-Like 1 (NPC1L1) sterol receptor on intestinal enterocytes and within the liver, ezetimibe blocks exogenous cholesterol absorption and has been shown to improve biochemical markers of NAFLD, improve insulin sensitivity and decrease hepatic steatosis. Ezetimibe 123-132 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 27-49 27714510-6 2016 By potently inhibiting the Niemann-Pick C1-Like 1 (NPC1L1) sterol receptor on intestinal enterocytes and within the liver, ezetimibe blocks exogenous cholesterol absorption and has been shown to improve biochemical markers of NAFLD, improve insulin sensitivity and decrease hepatic steatosis. Ezetimibe 123-132 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 51-57 26761771-7 2016 Cholesterol uptake was reduced by ezetimibe in L52P-NPC1L1, I300T-NPC1L1, but increased in S489G-NPC1L1 overexpressing cells. Ezetimibe 34-43 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 52-58 26761771-7 2016 Cholesterol uptake was reduced by ezetimibe in L52P-NPC1L1, I300T-NPC1L1, but increased in S489G-NPC1L1 overexpressing cells. Ezetimibe 34-43 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 66-72 26761771-7 2016 Cholesterol uptake was reduced by ezetimibe in L52P-NPC1L1, I300T-NPC1L1, but increased in S489G-NPC1L1 overexpressing cells. Ezetimibe 34-43 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 66-72 26761771-10 2016 Proteomic analyses identified increased association with proteins that modulate intermediate filament proteins in Comb-NPC1L1 versus WT-NPC1L1 treated with ezetimibe. Ezetimibe 156-165 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 119-125 26761771-10 2016 Proteomic analyses identified increased association with proteins that modulate intermediate filament proteins in Comb-NPC1L1 versus WT-NPC1L1 treated with ezetimibe. Ezetimibe 156-165 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 136-142 26934923-8 2016 On the other hand, its increased uptake was significantly inhibited by ezetimibe, a selective inhibitor of NPC1L1. Ezetimibe 71-80 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 107-113 26923679-6 2016 To date, ezetimibe represents the only inhibitor of NPC1L1 available for clinical use, however, novel aminoss- lactam ezetimibe derivatives have been synthesized and their efficacy to inhibit NPC1L1 protein and decrease plasma cholesterol levels is under evaluation. Ezetimibe 9-18 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 52-58 26923679-6 2016 To date, ezetimibe represents the only inhibitor of NPC1L1 available for clinical use, however, novel aminoss- lactam ezetimibe derivatives have been synthesized and their efficacy to inhibit NPC1L1 protein and decrease plasma cholesterol levels is under evaluation. Ezetimibe 9-18 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 192-198 26492642-13 2015 -762T > C and 1735C > G are two prevalent NPC1L1 variants which need further studies to explore their clinical impact on CHD prevalence and response to ezetimibe therapy in Chinese Hans. Ezetimibe 158-167 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 48-54 25589339-4 2015 Single nucleotide polymorphisms (SNPs) in NPC1L1 have been associated to variation in both plasma low-density lipoprotein (LDL) cholesterol levels and lipid-lowering medication with ezetimibe. Ezetimibe 182-191 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 42-48 25841872-1 2015 AIMS: Ezetimibe reduces plasma levels of low-density lipoprotein (LDL) cholesterol by inhibiting Niemann-Pick C1-Like protein 1 (NPC1L1), the transporter responsible for cholesterol uptake from the intestine into enterocytes and from the bile into hepatocytes. Ezetimibe 6-15 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 97-127 25841872-1 2015 AIMS: Ezetimibe reduces plasma levels of low-density lipoprotein (LDL) cholesterol by inhibiting Niemann-Pick C1-Like protein 1 (NPC1L1), the transporter responsible for cholesterol uptake from the intestine into enterocytes and from the bile into hepatocytes. Ezetimibe 6-15 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 129-135 25841872-2 2015 We tested the hypothesis that genetic variation in NPC1L1, mimicking the effect of ezetimibe, was associated with reduced risk of ischaemic vascular disease (IVD) and with increased risk of symptomatic gallstone disease. Ezetimibe 83-92 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 51-57 26442834-4 2015 Ezetimibe is a selective inhibitor of Niemann-Pick C1-like 1 (NPC1L1) protein that regulates the cholesterol uptake from the small intestine into the enterocytes. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 38-60 26442834-4 2015 Ezetimibe is a selective inhibitor of Niemann-Pick C1-like 1 (NPC1L1) protein that regulates the cholesterol uptake from the small intestine into the enterocytes. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 62-68 25589339-6 2015 Therefore, we assessed the contribution of two unexplored NPC1L1 variants on plasma lipids and response to ezetimibe in Chilean hypercholesterolemic individuals. Ezetimibe 107-116 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 58-64 25390462-1 2014 BACKGROUND: Ezetimibe lowers plasma levels of low-density lipoprotein (LDL) cholesterol by inhibiting the activity of the Niemann-Pick C1-like 1 (NPC1L1) protein. Ezetimibe 12-21 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 122-144 25551765-3 2014 In a screen for natural products that inhibit ezetimibe glucuronide binding to NPC1L1, we found a novel compound, fomiroid A, in extracts of the mushroom Fomitopsis nigra. Ezetimibe 46-55 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 79-85 25390462-1 2014 BACKGROUND: Ezetimibe lowers plasma levels of low-density lipoprotein (LDL) cholesterol by inhibiting the activity of the Niemann-Pick C1-like 1 (NPC1L1) protein. Ezetimibe 12-21 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 146-152 24861377-2 2014 Ezetimibe is known as an inhibitor for NPC1L1 and decreases concentration of low-density lipoprotein cholesterol (LDL-C) in blood. Ezetimibe 0-9 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 39-45 24906511-1 2014 Niemann-Pick type C1-like 1 (NPC1L1) is an intestinal cholesterol transporter that is known to be the target of the cholesterol absorption inhibitor ezetimibe. Ezetimibe 149-158 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-27 24906511-1 2014 Niemann-Pick type C1-like 1 (NPC1L1) is an intestinal cholesterol transporter that is known to be the target of the cholesterol absorption inhibitor ezetimibe. Ezetimibe 149-158 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 29-35 24906511-3 2014 Those steroid derivatives bound to a site different from both the sterol-binding domain and the ezetimibe-binding site, implying that they may be a novel class of NPC1L1 inhibitors with a distinct mode of action. Ezetimibe 96-105 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 163-169 23991401-3 2013 NPC1L1 is a molecular target of ezetimibe, an agent for hypercholesterolemia. Ezetimibe 32-41 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-6 24859282-1 2014 Niemann-Pick C1-Like 1 (NPC1L1) mediates cholesterol absorption, and ezetimibe is a potent NPC1L1 inhibitor applicable for medication of hypercholesterolemia. Ezetimibe 69-78 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 91-97 24214142-8 2014 CONCLUSION: Inhibition of NPC1L1 by ezetimibe activates autophagy in human hepatocytes by modulating cholesterol homeostasis. Ezetimibe 36-45 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 26-32 23830695-3 2013 Using this method, we discovered novel steroidal ligands of Niemann-Pick type C1-like 1 (NPC1L1), an intestinal cholesterol transporter that is the target of the cholesterol absorption inhibitor ezetimibe, and conducted structure-activity relationship studies. Ezetimibe 195-204 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 60-87 23830695-3 2013 Using this method, we discovered novel steroidal ligands of Niemann-Pick type C1-like 1 (NPC1L1), an intestinal cholesterol transporter that is the target of the cholesterol absorption inhibitor ezetimibe, and conducted structure-activity relationship studies. Ezetimibe 195-204 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 89-95 24974575-0 2014 The c.-133A > G polymorphism in NPC1L1 gene influences the efficacy of ezetimibe monotherapy on apolipoprotein A1 in hyperlipidemic patients. Ezetimibe 74-83 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 35-41 24974575-3 2014 To date effect of NPC1L1 c.-133A > G SNP on ezetimibe monotherapy has not been studied. Ezetimibe 47-56 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 18-24 24974575-4 2014 Our objective was to examine whether SNP c.-133A > G at the NPC1L1 gene has effects on lipid levels and on the efficacy of 3, 6 and 12 months of 10 mg daily ezetimibe monotherapy in hyperlipidemic patients with statin induced adverse effects. Ezetimibe 160-169 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 63-69 24974575-11 2014 NPC1L1-133A > G SNP influences the ApoA1 response to ezetimibe monotherapy, therefore, may alter the effect of ezetimibe on the structure and function of the high-density lipoprotein particles. Ezetimibe 56-65 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-6 24974575-11 2014 NPC1L1-133A > G SNP influences the ApoA1 response to ezetimibe monotherapy, therefore, may alter the effect of ezetimibe on the structure and function of the high-density lipoprotein particles. Ezetimibe 114-123 NPC1 like intracellular cholesterol transporter 1 Homo sapiens 0-6