Article
Extracellular loop C of NPC1L1 is important for binding to ezetimibe.
Proceedings of the National Academy of Sciences of the United States of America - 12 Aug 2008
Weinglass Adam B, Kohler Martin, Schulte Uwe, Liu Jessica, Nketiah Emmanuel O, Thomas Anu, Schmalhofer William, Williams Brande, Bildl Wolfgang, McMasters Daniel R, Dai Kevin, Beers Lindsey, McCann Margaret E, Kaczorowski Gregory J, Garcia Maria L
Abstract excerpt
Niemann-Pick C1-like protein (NPC1L1) mediates the absorption of dietary cholesterol in the proximal region of the intestine, a process that is blocked by cholesterol absorption inhibitors (CAIs), including ezetimibe (EZE). Using a proteomic approach, we demonstrate that NPC1L1 is the protein to which EZE and its analogs bind. Next, we determined the site of interaction of EZE analogs with NPC1L1 by exploiting...
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