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Estudio funcional del promotor del gen NPC1L1

Clínica e Investigación en Arteriosclerosis, 2008
Introduccion En la absorcion intestinal de colesterol intervienen distintos transportadores, uno de gran importancia y diana del farmaco ezetimiba, la proteina NPC1L1. Se ha demostrado una asociacion entre distintas variantes geneticas de NPC1L1, la eficiencia en la absorcion de esteroles y la concentracion plasmatica de colesterol unido a ...
Beatriz Martín   +5 more
openaire   +1 more source

Emodin lows NPC1L1-mediated cholesterol absorption as an uncompetitive inhibitor

Bioorganic & Medicinal Chemistry Letters, 2022
Emodin (EM) is one of the active components of the traditional Chinese medicine rhubarb, and there is evidence of its hypolipidemic activity, though the exact mechanism is unknown. NPC1L1 is a key protein in human cholesterol uptake that is primarily expressed in hepatocytes and gastrointestinal epithelial cells.
Jingsen, Meng   +8 more
openaire   +2 more sources

Hepatic NPC1L1 promotes hyperlipidemia in LDL receptor deficient mice

Biochemical and Biophysical Research Communications, 2018
Niemann-Pick C1-like1 (NPC1L1), a crucial cholesterol absorption receptor expressed in human intestine and liver. But in mouse it is only expressed in intestine. Previous studies elucidated that expression of human NPC1L1 in mouse liver led to increase of plasma cholesterol due to activation of absorption from bile. However, hepatic NPC1L1 function was
Youlin Wang   +4 more
openaire   +2 more sources

In Vivo Responsiveness to Ezetimibe Correlates with Niemann-Pick C1 Like-1 (NPC1L1) Binding Affinity: Comparison of Multiple Species NPC1L1 Orthologs

Molecular Pharmacology, 2007
Ezetimibe is the first in class 2-azetidinone that decreases plasma cholesterol by blocking intestinal cholesterol absorption. Ezetimibe effectively reduces plasma cholesterol in several species including human, monkey, dog, hamster, rat, and mouse, but the potency ranges widely.
Brian E, Hawes   +6 more
openaire   +2 more sources

NPC1L1: from drug target to physiological sterol transporter

Future Lipidology, 2006
‘In less than 3 years, NPC1L1 has skyrocketed from virtually unknown status to becoming a key player in normal physiology’
Rebecca Pollex, Robert Hegele
openaire   +1 more source

Sequencing of a npc1L1 mutation in larval zebrafish

Proceedings of the West Virginia Academy of Science, 2020
NPC1L1 transport protein is located in the lumen of the intestines and is critical for cholesterol absorption. The reason why we study NPC1L1 is because cholesterol absorption in the intestines affect obesity and diabetes which is still under investigation.
Jordan Marcelle Smith   +2 more
openaire   +1 more source

Frequent Cholesterol Intake Up-regulates Intestinal NPC1L1, ACAT2, and MTP

Journal of Agricultural and Food Chemistry, 2010
Dietary cholesterol elevates plasma total cholesterol (TC) level. However, no study to date has examined how cholesterol intake frequency interacts with the gene of sterol transporters, receptors, and enzymes involved in cholesterol metabolism. Thirty-three hamsters were divided into three groups with the control hamsters being given daily 9 mg of ...
Rui, Jiao   +7 more
openaire   +2 more sources

Transporters as Drug Targets: Discovery and Development of NPC1L1 Inhibitors

Clinical Pharmacology & Therapeutics, 2009
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. The NPC1L1 protein mediates sterol transport across the enterocyte brush border membrane and is essential for intestinal cholesterol ...
J L, Betters, L, Yu
openaire   +2 more sources

Niemann–Pick C1 Like 1 (NPC1L1) an intestinal sterol transporter

Biochimica Et Biophysica Acta - Molecular and Cell Biology of Lipids, 2009
Niemann-Pick C1 Like 1 (NPC1L1) has been identified and characterized as an essential protein in the intestinal cholesterol absorption process. NPC1L1 localizes to the brush border membrane of absorptive enterocytes in the small intestine. Intestinal expression of NPC1L1 is down regulated by diets containing high levels of cholesterol.
Harry R, Davis, Scott W, Altmann
exaly   +3 more sources

Dual targeting PPARα and NPC1L1 metabolic vulnerabilities blocks tumorigenesis

Cancer Letters
Dysregulated lipid metabolism is linked to tumor progression. In this study, we identified Niemann-Pick C1-like 1 (NPC1L1) as a downstream effector of PKM2. In breast cancer cells, PKM2 knockout (KO) enhanced NPC1L1 expression while downregulating peroxisome proliferator-activated receptor α (PPARα) signaling pathway.
Xiaona You   +15 more
openaire   +2 more sources

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