RETINOIC ACID AND SYNTHETIC ANALOGS DIFFERENTIALLY ACTIVATE RETINOIC ACID RECEPTOR DEPENDENT TRANSCRIPTION

被引：90

作者：

ASTROM, A ^{[1
]}

PETTERSSON, U ^{[1
]}

KRUST, A ^{[1
]}

CHAMBON, P ^{[1
]}

VOORHEES, JJ ^{[1
]}

机构：

[1] FAC MED STRASBOURG,CNRS,GENET MOLEC EUCARYOTES LAB,INSERM,U184,STRASBOURG,FRANCE

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1990年 / 173卷 / 01期

关键词：

D O I：

10.1016/S0006-291X(05)81062-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We have developed an assay where the potency of retinoids in retinoic acid receptor (RAR) mediated transcriptional activation can be rapidly evaluated. In this assay hRAR-α, hRAR-β and hRAR-γ were expressed in CV-1 cells together with a reporter gene containing a retinoic acid responsive element (TRE3-tk-CAT). Concentrations required to obtain half-maximum induction (ED50 of CAT-activity were determined for several retinoids, e.g., all-trans-retinoic acid (RA), 13-cis-retinoic acid (13-cis-RA), arotinoid acid (TTNPB) and m-carboxy-arotinoid acid (m-carboxy-TTNPB, an inactive arotinoid analog). The ED50 values for RA decreased in the order of RAR-α (24 nM) > RAR-β (4.0 nM) > RAR-γ (1.3 nM), while the ED50 values for TTNPB and 13-cis-RA decreased in the order of RAR-α (6.5 nM, 190 nM) > RAR-γ (2.3 nM, 140 nM) > RAR-β (0.6 nM, 43 nM), respectively. No significant inductions were obtained when cells were treated with m-carboxy-TTNPB, even at 10 μM concentrations. The fold induction of CAT-activity for all compounds tested decreased in the order of RAR-α > RAR-β > RAR-γ. © 1990 Academic Press, Inc.

引用

页码：339 / 345

页数：7

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