RETINOIDS SELECTIVE FOR RETINOID-X RECEPTOR RESPONSE PATHWAYS
RETINOIDS SELECTIVE FOR RETINOID-X RECEPTOR RESPONSE PATHWAYS
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DOI：
10.1126/science.1335166
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发表时间：
1992-12-18
期刊：
影响因子：
56.9
通讯作者：
PFAHL, M
中科院分区：
文献类型：
--
作者：
LEHMANN, JM;JONG, L;PFAHL, M
类维生素A具有广泛的生物活性，是有用的治疗剂。它们的生理活性由两种类型的受体介导，视黄酸受体（RAR）和类维生素A X受体（RXR）。RAR以及几种相关受体需要与RXR异源二聚化以实现有效的DNA结合和功能。然而，在存在9-顺式视黄酸（RAR和RXR的配体）的情况下，RXR也可以形成同二聚体。据报道，一系列类维生素A选择性激活RXR同源二聚体，但不影响RAR-RXR异源二聚体，因此证明两种类维生素A反应途径都可以独立激活。
Retinoids have a broad spectrum of biological activities and are useful therapeutic agents. Their physiological activities are mediated by two types of receptors, the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs). RARs, as well as several related receptors, require heterodimerization with RXRs for effective DNA binding and function. However, in the presence of 9-cis-retinoic acid, a ligand for both RARs and RXRs, RXRs can also form homodimers. A series of retinoids is reported that selectively activates RXR homodimers but does not affect RAR-RXR heterodimers and thus demonstrates that both retinoid response pathways can be independently activated.