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Two panels of steroid receptor luciferase reporter cell lines for compound profiling
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SYSNO ASEP 0365123 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Two panels of steroid receptor luciferase reporter cell lines for compound profiling Author(s) Sedlák, David (UMG-J) RID
Paguio, A. (US)
Bartůněk, Petr (UMG-J) RIDSource Title Combinatorial Chemistry & High Throughput Screening - ISSN 1386-2073
Roč. 14, č. 2 (2011), s. 248-266Number of pages 9 s. Language eng - English Country NL - Netherlands Keywords nuclear hormone receptor ; steroid receptor ; cell-based luciferase reporter assay Subject RIV EB - Genetics ; Molecular Biology R&D Projects LC06077 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z50520514 - UMG-J (2005-2011) UT WOS 000290611700003 DOI 10.1182/blood-2011-01-331199 Annotation Here we describe the creation of two panels of luciferase reporter cell lines for estrogen receptors α and β, androgen, glucocorticoid, mineralocorticoid and progesterone receptors. In the first panel, the activation of synthetic, multiple response elements containing, luciferase reporter or viral promoter derived from MMTV LTR is mediated by full-length exogenously expressed receptors. The second panel relies on the expression of the chimeric receptor created by the replacement of the N-terminal part of the molecule by Gal4 DBD. The profiling of both systems with 28 ligands generated qualitatively similar response in terms of potency, efficacy, partial agonism/antagonism, mixed agonistic/antagonistic profiles etc., and the rank of potencies was well conserved between both panels. However, we have also identified artifacts introduced by the Gal4/LBD reporters in contrast to their full-length receptor reporter counterparts such as the agonist/antagonist transition of some MR agonists. Workplace Institute of Molecular Genetics Contact Nikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217 Year of Publishing 2012
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