Abstract
Screening of bona fide ligands for nuclear receptors is a real tour de force as the identified molecules are supposed to be able to activate the targeted proteins in cell culture as well as in vivo. Indeed orphan nuclear receptors are putative pharmacologically targets for various diseases. It is thus necessary to have quick and reproductive systems that help in identifying new ligands, agonist or antagonist, before using them in vivo in animal models to check for secondary effects. Here, we describe the transient transfections (homologous and heterologous) used for the screening of ligands for liver X receptor α (LXRα, NR1H3) in HeLa cells.
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References
Peet DJ, Janowski BA, Mangelsdorf DJ (1998) The LXRs: a new class of oxysterol receptors. Curr Opin Genet Dev 8:571–575
Peet DJ et al (1998) Cholesterol and bile acid metabolism are impaired in mice lacking the nuclear oxysterol receptor LXR alpha. Cell 93:693–704
Viennois E et al (2012) Selective liver X receptor modulators (SLiMs): what use in human health? Mol Cell Endocrinol 351:129–141
Bookout AL et al (2006) Anatomical profiling of nuclear receptor expression reveals a hierarchical transcriptional network. Cell 126:789–799
Janowski BA, Willy PJ, Devi TR, Falck JR, Mangelsdorf DJ (1996) An oxysterol signalling pathway mediated by the nuclear receptor LXR alpha. Nature 383:728–731
Janowski BA et al (1999) Structural requirements of ligands for the oxysterol liver X receptors LXRalpha and LXRbeta. Proc Natl Acad Sci U S A 96:266–271
Viennois E et al (2011) Targeting liver X receptors in human health: deadlock or promising trail? Expert Opin Ther Targets 15:219–232
Volle DH et al (2004) Regulation of the aldo-keto reductase gene akr1b7 by the nuclear oxysterol receptor LXRalpha (liver X receptor-alpha) in the mouse intestine: putative role of LXRs in lipid detoxification processes. Mol Endocrinol 18:888–898
Brand AH, Perrimon N (1993) Targeted gene expression as a means of altering cell fates and generating dominant phenotypes. Development 118:401–415
Willy PJ, Mangelsdorf DJ (1997) Unique requirements for retinoid-dependent transcriptional activation by the orphan receptor LXR. Genes Dev 11:289–298
Kaneko E et al (2003) Induction of intestinal ATP-binding cassette transporters by a phytosterol-derived liver X receptor agonist. J Biol Chem 278:36091–36098
Repa JJ et al (2000) Regulation of mouse sterol regulatory element-binding protein-1c gene (SREBP-1c) by oxysterol receptors, LXRalpha and LXRbeta. Genes Dev 14:2819–2830
Acknowledgements
This work was supported by grants from Fondation BNP-Paris, Région Auvergne, Fond Européen de Développement Régional (FEDER), Association de Recherche sur les Tumeurs Prostatiques (ARTP), Fondation ARC, Ligue contre le Cancer for JMAL and CB, Conférence Episcopale Italienne, Union Economique Monétaire Ouest Africaine (UEMOA), and Campus France for BB. We thank David J. Mangelsdorf (Howard Hughes Medical Institute, Dallas, TX) and M. Makishima (Nihon University School of Medicine, Tokyo, Japan) for plasmids.
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Lobaccaro, JM.A., Beaudoin, C., Bayala, B., Baron, S., Trousson, A. (2016). Lipid Homeostasis and Ligands for Liver X Receptors: Identification and Characterization. In: McEwan, PhD, I. (eds) The Nuclear Receptor Superfamily. Methods in Molecular Biology, vol 1443. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-3724-0_2
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DOI: https://doi.org/10.1007/978-1-4939-3724-0_2
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