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首页> 外文期刊>Molecular and Cellular Biology >Role of the ligand in intracellular receptor function: receptor affinity determines activation in vitro of the latent dioxin receptor to a DNA-binding form.
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Role of the ligand in intracellular receptor function: receptor affinity determines activation in vitro of the latent dioxin receptor to a DNA-binding form.

机译：配体在细胞内受体功能中的作用：受体亲和力决定了潜在的二恶英受体在体外活化成DNA结合形式。

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摘要

To reconstitute the molecular mechanisms underlying the cellular response to soluble receptor ligands, we have exploited a cell-free system that exhibits signal- (dioxin-)induced activation of the latent cytosolic dioxin receptor to an active DNA-binding species. The DNA-binding properties of the in vitro-activated form were qualitatively indistinguishable from those of in vivo-activated nuclear receptor extracted from dioxin-treated cells. In vitro activation of the receptor by dioxin was dose dependent and was mimicked by other dioxin receptor ligands in a manner that followed the rank order of their relative affinities for the receptor in vitro and their relative potencies to induce target gene transcription in vivo. Thus, in addition to triggering the initial release of inhibition of DNA binding and presumably allowing nuclear translocation, the ligand appears to play a crucial role in the direct control of the level of functional activity of a given ligand-receptor complex.
机译：为了重建潜在的细胞对可溶性受体配体反应的分子机制，我们开发了一种无细胞系统，该系统表现出信号（二恶英）诱导的潜在胞质二恶英受体向活性DNA结合物种的激活。体外活化形式的DNA结合特性与从二恶英处理过的细胞中提取的体内活化核受体的特性在质量上没有区别。二恶英在体外对受体的激活是剂量依赖性的，并被其他二恶英受体配体模仿，其方式是按照其对受体的相对亲和力及其在体内诱导靶基因转录的相对能力的顺序排列。因此，除了触发对DNA结合的抑制作用的最初释放并可能允许核易位外，配体似乎在直接控制给定配体-受体复合物的功能活性水平中起着关键作用。

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