In the classic model of nuclear receptor signaling, specific hormone binding results in the recruitment of coactivator proteins and transcriptional activation. Recent results with newly characterized nuclear receptors have expanded this model to include new types of ligands and novel transcriptional responses. Both inverse agonists and conventional agonist ligands have been identified for the xenobiotic receptor constitutive androstane receptor (CAR), a constitutive activator of transcription in the absence of ligands.
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New insights into the regulation of cyp3a65 expression in transgenic tg(cyp3a65:GFP) zebrafish embryos.
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Unité écotoxicologie des substances et des milieux, Institut National de l'Environnement Industriel et des Risques (INERIS), 60550 Verneuil-en-Halatte, France. Electronic address:
Facing the need for alternative models allowing assessment of metabolic-endocrine disrupting chemicals (MDCs), especially in poorly investigated tissues such as the intestine, we recently developed a transgenic zebrafish embryo in vivo model, tg(cyp3a65:GFP), expressing the Green Fluorescent Protein (GFP) under the control of the zebrafish cyp3a65 promoter, ortholog of human cyp3a4, a gene coding for a key enzyme of intestinal xenobiotic and endobiotic metabolism. In this study, we aimed to better understand the regulation of cyp3a65 expression by zfPXR, zfAhR2, and zfGR zebrafish orthologs of well-known human xenosensors PXR and AhR, and steroid nuclear receptor GR. For this purpose, we performed zebrafish embryo tg(cyp3a65:GFP) (co)exposures to a variety of agonists (clotrimazole, TCDD, fluticasone propionate) and antagonists (econazole nitrate, CH223181, RU486), which were characterized using in vitro zebrafish reporter gene assays.
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