Cholesterol homeostasis by the intestine: Lessons from Niemann-Pick C1 Like 1 [NPC1L1)

Atherosclerosis Supplements

Volumn 9, Issue 2, 2008, Pages 77-81

  Davis Jr , Harry R ^a   Basso, Federica ^a   Hoos, Lizbeth M ^a   Tetzloff, Glen ^a   Lally, Sean M ^a   Altmann, Scott W ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cholesterol absorption inhibitor; Cholesterol transporter; Ezetimibe; NPC1L1

Indexed keywords

APOLIPOPROTEIN B48; APOLIPOPROTEIN E; CHOLESTEROL; CHYLOMICRON REMNANT; EZETIMIBE; PHYTOSTEROL; PROTEIN; PROTEIN NPC1L1; SCAVENGER RECEPTOR BI; STEROL; UNCLASSIFIED DRUG;

ARTICLE; ATHEROSCLEROSIS; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL METABOLISM; CHOLESTEROL TRANSPORT; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG TARGETING; HYPERCHOLESTEROLEMIA; INTESTINE; LIPID ABSORPTION; NONHUMAN; PRIORITY JOURNAL; PROTEIN FUNCTION;

ANIMALS; ANTICHOLESTEREMIC AGENTS; ATHEROSCLEROSIS; AZETIDINES; CHOLESTEROL; CHOLESTEROL, DIETARY; DISEASE PROGRESSION; HUMANS; INTESTINAL ABSORPTION; INTESTINES;

EID: 50849115476     PISSN: 15675688     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.atherosclerosissup.2008.05.008     Document Type: Article

References (22)

1. Clader J. The discovery of ezetimibe: a view from outside the receptor. J Med Chem 47 1 (2004) 1-9
2. Ballantyne C.M. Ezetimibe: efficacy and safety in clinical trials. Eur Heart J 4 Suppl J (2002) J9-J18
3. Sybertz E.J., Davis H.R., Van Heek M., et al. SCH48461, a novel inhibitor of cholesterol absorption. In: Woodford F.P., Davignon J., and Sniderman A. (Eds). Atherosclerosis X (1995), Elsevier 311-315
4. van Heek M., Farley C., Compton D.S., Hoos L., and Davis H.R. Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function. Br J Pharm 134 (2001) 409-417
5. van Heek M., Compton D.S., and Davis H.R. The cholesterol absorption inhibitor, ezetimibe, decreases diet-induced hypercholesterolemia in monkeys. Eur J Pharm 415 (2001) 79-84
6. Sudhop T., Lutjohann D., Kodal A., et al. Inhibition of cholesterol absorption by ezetimibe in humans. Circulation 106 (2002) 1943-1948
7. Clarenbach J.J., Reber M., Lutjohann D., von Bergmann K., and Sudhop T. The lipid-lowering effect of ezetimibe in pure vegetarians. J Lipid Res 47 12 (2006) 2820-2824
8. Staprans I., Pan X.-M., Rapp J.H., Moser A.H., and Feingold K.R. Ezetimibe inhibits the incorporation of dietary oxidized cholesterol into lipoproteins. J Lipid Res 47 (2006) 2575-2580
9. Altmann S.W., Davis H.R., Zhu L., et al. Niemann-Pick C1 Like 1 protein is critical for intestinal cholesterol absorption. Science 303 (2004) 1201-1204
10. Iyer S.N., Yao X., Crona J.H., et al. Characterization of the putative and recombinant rat sterol transporter Niemann-Pick C1 Like 1 (NPC1L1) protein. Biochim Biophys Acta 1722 3 (2005) 282-292
11. Davis H.R., Zhu L., Hoos L.M., et al. Niemann-Pick C1 Like 1 (NPC1L1) is the intestinal phytosterol and cholesterol transporter and a key modulator of whole body cholesterol homeostasis. J Biol Chem 279 32 (2004) 33486-33592
12. Dixit S.S., Sleat D.E., Stock A.M., and Lobel P. Do mammalian NPC1 and NPC2 play a role in Intestinal cholesterol absorption?. Biochem J 408 (2007) 1-5
13. Lally S.M., Hoos L.M., Maguire M., et al. Intestinal cholesterol uptake in SR-B1 and Niemann-Pick C1 Like 1 knockout mice. Arterioscler Thromb Vasc Biol 27 (2007) e85
14. Huff M.W., Pollex R.L., and Hegele R.A. NPC1L1: Evolution from pharmacological target to physiological sterol transporter. Arterioscler Thromb Vasc Biol 26 (2006) 2433-2438
15. Salen G., et al., Multicenter Sitosterolemia Study Group. Ezetimibe effectively reduces plasma plant sterols in patients with sitosterolemia. Circulation 109 8 (2004) 966-971
16. Davis H.R., Compton D., Hoos L., and Tetzloff G. Ezetimibe, a potent cholesterol absorption inhibitor, inhibits the development of atherosclerosis in apoE knockout mice. Arterioscler Thromb Vasc Biol 21 (2001) 2032-2038
17. Davis H.R., Hoos L.M., Tetzloff G., et al. Deficiency of Niemann-Pick C1 Like 1 (NPC1L1) prevents atherosclerosis in apoE -/- mice. Arterioscler Thromb Vasc Biol 27 (2007) 841-849
18. Labonte E.D., Howles P.N., Norman G.A., et al. Class B type I scavenger receptor is responsible for the high affinity cholesterol binding activity of intestinal brush border membrane vesicles. Biochim Biophys Acta 1771 (2007) 1132-1139
19. Garcia-Calvo M., Lisnock J., Bull H.G., et al. The target of ezetimibe is Niemann-Pick C1 Like 1 (NPC1L1). Proc Natl Acad Sci USA 102 23 (2005) 8132-8137
20. Hawes B.E., O'Neill K.A., Yao X., et al. In vivo responsiveness to ezetimibe correlates with NPC1L1 binding affinity: comparison of multiple species NPC1L1 orthologs. Mol Pharmacol 71 1 (2007) 19-29
21. Yu L., Bharadwaj S., Brown J.M., et al. Cholesterol-regulated translocation of NPC1L1 to the cell surface facilitates free cholesterol uptake. J Biol Chem 281 (2006) 6616-6624
22. Cohen J.C., Pertsemlidis A., Fahmi S., et al. Multiple rare variants in NPC1L1 associated with reduced sterol absorption and plasma low-density lipoprotein levels. Proc Natl Acad Sci USA 103 6 (February 7) (2006) 1810-1825