NPC1L1 binds ezetimibe

Stable Identifier
Reaction [binding]
Homo sapiens
NPC1L1 inactivation by ezetimibe, NPC1L1 + ezetimibe => NPC1L1:ezetimibe complex
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Human NPC1L1, associated with the plasma membrane, binds ezetimibe and becomes incapable of mediating cholesterol uptake. The molecular mechanisms of cholesterol transport and ezetimibe inhibition, however, remain unclear (Garcia-Calvo et al. 2005; Weinglass et al. 2008).

Literature References
PubMed ID Title Journal Year
18187582 Madin-Darby canine kidney II cells: a pharmacologically validated system for NPC1L1-mediated cholesterol uptake

Beers, L, Nketiah, EO, Thomas, A, Schmalhofer, W, Williams, B, Köhler, MG, Bleasby, K, Leone, J, Hafey, M, Smith, L, Kaczorowski, GJ, Garcia, ML, Braun, MP, Tang, YS, Ujjainwalla, F, Liu, J, McCann, ME, Weinglass, AB

Mol Pharmacol 2008
15928087 The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)

Lisnock, J, Garcia-Calvo, M, Shevell, DE, Iyer, SP, Chapman, KT, Smith, MM, Altmann, SW, Detmers, PA, Ogawa, A, Thornberry, NA, Dean, DC, Bull, HG, Crona, JH, Davis HR, Jr, O'Neill, KA, Graziano, MP, Makarewicz, AM, Braun, MP, Hughes, M, Tang, YS, Hawes, BE, Ujjainwalla, F, Macintyre, DE, Burnett, DA

Proc Natl Acad Sci U S A 2005
Orthologous Events
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