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Two panels of steroid receptor luciferase reporter cell lines for compound profiling
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SYSNO ASEP 0365123 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Two panels of steroid receptor luciferase reporter cell lines for compound profiling Tvůrce(i) Sedlák, David (UMG-J) RID
Paguio, A. (US)
Bartůněk, Petr (UMG-J) RIDZdroj.dok. Combinatorial Chemistry & High Throughput Screening - ISSN 1386-2073
Roč. 14, č. 2 (2011), s. 248-266Poč.str. 9 s. Jazyk dok. eng - angličtina Země vyd. NL - Nizozemsko Klíč. slova nuclear hormone receptor ; steroid receptor ; cell-based luciferase reporter assay Vědní obor RIV EB - Genetika a molekulární biologie CEP LC06077 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy CEZ AV0Z50520514 - UMG-J (2005-2011) UT WOS 000290611700003 DOI 10.1182/blood-2011-01-331199 Anotace 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. Pracoviště Ústav molekulární genetiky Kontakt Nikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217 Rok sběru 2012
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