NPC1L1 inactivation by ezetimibe

Stable Identifier
R-HSA-265456
Type
Reaction [binding]
Species
Homo sapiens
Compartment
Synonyms
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
15928087 The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)

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

Proc Natl Acad Sci U S A 2005
18187582 Madin-Darby canine kidney II cells: a pharmacologically validated system for NPC1L1-mediated cholesterol uptake

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

Mol Pharmacol 2008
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