9-CIS RETINOIC ACID IS A HIGH-AFFINITY LIGAND FOR THE RETINOID-X RECEPTOR
9-CIS RETINOIC ACID IS A HIGH-AFFINITY LIGAND FOR THE RETINOID-X RECEPTOR
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DOI：
10.1016/0092-8674(92)90479-v
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发表时间：
1992-01-24
期刊：
影响因子：
64.5
通讯作者：
THALLER, C
中科院分区：
文献类型：
--
作者：
HEYMAN, RA;MANGELSDORF, DJ;THALLER, C
全反式视黄酸（RA）以前已被证明可以调节视黄酸受体（RAR）和类维生素A X受体（RXR）的转录特性。全反式RA不能与RXR结合，表明它可能被代谢为更活跃的高亲和力配体。我们在这里报告的实验方法，已确定9-顺式RA作为RXR配体。在转染试验中，它的效力比全反式RA高40倍，并以高亲和力结合。9-顺式RA在培养细胞中的产生以及该分子在肝脏和肾脏中的鉴定证明了该分子在活生物体中的存在。这种新激素的发现指出了类维生素A代谢在产生新信号通路中的关键作用。
All-trans retinoic acid (RA) has previously been shown to modulate the transcriptional properties of the retinoic acid receptor (RAR) and retinoid X receptor (RXR). The inability of all-trans RA to bind to RXR suggests that it may be metabolized to a more active high affinity ligand. We report here an experimental approach that has identified 9-cis RA as an RXR ligand. It is up to 40-fold more potent than all-trans RA in transfection assays and binds with high affinity. The production of 9-cis RA in cultured cells and the identification of this molecule in liver and kidney demonstrates the existence of this molecule in living organisms. The discovery of this novel hormone points to the key role retinoid metabolism may have in generating new signaling pathways.