title: Intestinal cholesterol transport proteins: an update and beyond.
abstract: OBJECTIVE
  Various studies have delineated the causal role of dietary cholesterol in atherogenesis. Strategies have thus been developed to minimize cholesterol absorption, and cholesterol transport proteins found at the apical membrane of enterocytes have been extensively investigated. This review focuses on recent progress related to various brush-border proteins that are potentially involved in alimentary cholesterol transport.
  
  
  RESULTS
  Molecular mechanisms responsible for dietary cholesterol and plant sterol uptake have not been completely defined. Growing evidence, however, supports the concept that several proteins are involved in mediating intestinal cholesterol transport, including SR-BI, NPC1L1, CD36, aminopeptidase N, P-glycoprotein, and the caveolin-1/annexin-2 heterocomplex. Other ABC family members (ABCA1 and ABCG5/ABCG8) act as efflux pumps favoring cholesterol export out of absorptive cells into the lumen or basolateral compartment. Several of these cholesterol carriers influence intracellular cholesterol homeostasis and are controlled by transcription factors, including RXR, LXR, SREBP-2 and PPARalpha. The lack of responsiveness of NPC1L1-deficient mice to ezetimibe suggests that NPC1L1 is likely to be the principal target of this cholesterol-lowering drug.
  
  
  CONCLUSIONS
  The understanding of the role, genetic regulation and coordinated function of proteins mediating intestinal cholesterol transport may lead to novel ways of treating cardiovascular disease.
authors.affiliation: Research Centre, CHU-Sainte-Justine, Québec, Canada. emile.levy@recherche-ste-justine.qc.ca
authors.forename: Emile
authors.initials: E
authors.lastname: Levy
authors.forename: Schohraya
authors.initials: S
authors.lastname: Spahis
authors.forename: Daniel
authors.initials: D
authors.lastname: Sinnett
authors.forename: Noel
authors.initials: N
authors.lastname: Peretti
authors.forename: Françoise
authors.initials: F
authors.lastname: Maupas-Schwalm
authors.forename: Edgard
authors.initials: E
authors.lastname: Delvin
authors.forename: Marie
authors.initials: M
authors.lastname: Lambert
authors.forename: Marc-André
authors.initials: MA
authors.lastname: Lavoie
mesh_terms: D000818:Animals; D017306:Annexin A2 / Q000378:metabolism*; D000924:Anticholesteremic Agents / Q000494:pharmacology; D050197:Atherosclerosis / Q000378:metabolism; D001692:Biological Transport; D018955:CD36 Antigens / Q000378:metabolism*; D051242:Caveolin 1 / Q000378:metabolism*; D002784:Cholesterol / Q000378:metabolism*; D002791:Cholesterol, Dietary / Q000378:metabolism; D004032:Diet; D006801:Humans; D008871:Microvilli / Q000378:metabolism; D008954:Models, Biological; D013261:Sterols / Q000737:chemistry
chemical_list: C472822:ANXA2 protein, human; D017306:Annexin A2; D000924:Anticholesteremic Agents; D018955:CD36 Antigens; D051242:Caveolin 1; D002791:Cholesterol, Dietary; D013261:Sterols; D002784:Cholesterol