Počet záznamů: 1

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

  1. 1.
    0365123 - UMG-J 2012 RIV NL eng J - Článek v odborném periodiku
    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
    Grant CEP: GA MŠk(CZ) LC06077
    Výzkumný záměr: CEZ:AV0Z50520514
    Klíčová slova: nuclear hormone receptor * steroid receptor * cell-based luciferase reporter assay
    Kód oboru RIV: EB - Genetika a molekulární biologie
    Impakt faktor: 1.785, rok: 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.
    Trvalý link: http://hdl.handle.net/11104/0200439