Abstract
Reporter gene assays are critical tools of nuclear receptor research for characterizing the effects of ligands on nuclear receptor activity. Common luciferase-based techniques require expensive substrates and are typically performed in endpoint format. Here, we describe a versatile reporter gene assay to observe nuclear receptor activity with fluorescent proteins as reporters. This setting is highly cost-efficient and enables observation of nuclear receptor activity over time with multiple measurements from one plate.
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References
Germain P, Staels B, Dacquet C, Spedding M, Laudet V (2006) Overview of nomenclature of nuclear receptors. Pharmacol Rev 58:685–704. https://doi.org/10.1124/pr.58.4.2
Aranda A, Pascual A (2001) Nuclear hormone receptors and gene expression. Physiol Rev 81:1269–1304
Benoit G, Cooney A, Giguere V, Ingraham H, Lazar M, Muscat G, Perlmann T, Renaud JP, Schwabe J, Sladek F, Tsai MJ, Laudet V (2006) International union of pharmacology. LXVI. Orphan nuclear receptors. Pharmacol Rev 58:798–836. https://doi.org/10.1124/pr.58.4.10
Merk D, Steinhilber D, Schubert-Zsilavecz M (2014) Characterizing ligands for farnesoid X receptor-available in vitro test systems for farnesoid X receptor modulator development. Expert Opin Drug Discov 9:27–37. https://doi.org/10.1517/17460441.2014.860129
Heering J, Merk D (1966) Hybrid reporter gene assays: versatile in vitro tools to characterize nuclear receptor modulators. Methods Mol Biol 2019:175–192. https://doi.org/10.1007/978-1-4939-9195-2_14
Gellrich L, Heitel P, Heering J, Kilu W, Pollinger J, Goebel T, Kahnt A, Arifi S, Pogoda W, Paulke A, Steinhilber D, Proschak E, Wurglics M, Schubert-Zsilavecz M, Chaikuad A, Knapp S, Bischoff I, Fürst R, Merk D (2020) L-thyroxin and the nonclassical thyroid hormone TETRAC are potent activators of PPARÎ. J Med Chem 63:6727–6740. https://doi.org/10.1021/acs.jmedchem.9b02150
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Schallmayer, E., Merk, D. (2023). A Fluorescence-Based Reporter Gene Assay to Characterize Nuclear Receptor Modulators. In: Merk, D., Chaikuad, A. (eds) Chemogenomics. Methods in Molecular Biology, vol 2706. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-3397-7_9
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DOI: https://doi.org/10.1007/978-1-0716-3397-7_9
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Online ISBN: 978-1-0716-3397-7
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