Two panels of steroid receptor luciferase reporter cell lines for compound profiling

0365123 - ÚMG 2012 RIV NL eng J - Journal Article
Sedlák, David - Paguio, A. - Bartůněk, Petr
Two panels of steroid receptor luciferase reporter cell lines for compound profiling.
Combinatorial Chemistry & High Throughput Screening. Roč. 14, č. 2 (2011), s. 248-266. ISSN 1386-2073. E-ISSN 1875-5402
R&D Projects: GA MŠMT(CZ) LC06077
Institutional research plan: CEZ:AV0Z50520514
Keywords : nuclear hormone receptor * steroid receptor * cell-based luciferase reporter assay
Subject RIV: EB - Genetics ; Molecular Biology
Impact factor: 1.785, year: 2011

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.
Permanent Link: http://hdl.handle.net/11104/0200439