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

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. One potential facto...

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Veröffentlicht in:	Molecular pharmacology 2007-01, Vol.71 (1), p.19-29
Hauptverfasser:	Hawes, Brian E., O’Neill, Kim A., Yao, Xiaorui, Crona, James H., Davis, Harry R., Graziano, Michael P., Altmann, Scott W.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Animals Anticholesteremic Agents - pharmacology Azetidines - pharmacokinetics Azetidines - pharmacology Binding Sites Cells, Cultured Cholesterol - metabolism Cloning, Molecular DNA, Complementary - genetics Ezetimibe Humans Intestinal Absorption Membrane Proteins - chemistry Membrane Proteins - genetics Membrane Proteins - physiology Models, Molecular Molecular Sequence Data Niemann-Pick Diseases Protein Conformation Rats
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