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首页> 外文期刊>Nature >Activation of specific RXR heterodimers by an antagonist of RXR homodimers.
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Activation of specific RXR heterodimers by an antagonist of RXR homodimers.

机译：RXR同二聚体的拮抗剂激活特定的RXR异二聚体。

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摘要

Retinoid X receptor (RXR) plays a central role in the regulation of many intracellular receptor signalling pathways and can mediate ligand-dependent transcription, acting as a homodimer or as a heterodimer. Here we identify an antagonist towards RXR homodimers which also functions as an agonist when RXR is paired as a heterodimer to specific partners, including peroxisome proliferator-activated receptor and retinoic acid receptor. This dimer-selective ligand confers differential interactions on the transcription machinery: the antagonist promotes association with TAF110 (TATA-binding protein (TBP)-associated factor 110) and the co-repressor SMRT, but not with TBP, and these properties are distinct from pure RXR agonists. This unique class of RXR ligands will provide a means to control distinct target genes at the level of transcription and allow the development of retinoids with a new pharmacological action.
机译：类视黄醇X受体（RXR）在许多细胞内受体信号传导途径的调节中起着核心作用，并且可以介导配体依赖性转录，作为同二聚体或异二聚体。在这里，我们确定了针对RXR同型二聚体的拮抗剂，当RXR与异型二聚体配对时，它也可以作为激动剂与特定的伴侣配对，包括过氧化物酶体增殖物激活受体和视黄酸受体。这种二聚体选择性配体赋予了转录机制不同的相互作用：拮抗剂促进与TAF110（TATA结合蛋白（TBP）相关因子110）和共阻遏物SMRT的结合，但不与TBP结合，这些特性与纯RXR激动剂。这类独特的RXR配体将提供一种在转录水平上控制不同靶基因的方法，并允许以新药理作用开发类维生素A。

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