A RETINOIC ACID RECEPTOR-ALPHA ANTAGONIST SELECTIVELY COUNTERACTS RETINOIC ACID EFFECTS
A RETINOIC ACID RECEPTOR-ALPHA ANTAGONIST SELECTIVELY COUNTERACTS RETINOIC ACID EFFECTS
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DOI：
10.1073/pnas.89.15.7129
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发表时间：
1992-08-01
影响因子：
11.1
通讯作者：
KLAUS, M
中科院分区：
文献类型：
--
作者：
APFEL, C;BAUER, F;KLAUS, M
视黄酸（RA）通过激活转录因子家族RA受体（RARs）对细胞的生长和分化发挥多效性作用。这些受体存在三种亚型，RAR-α、RAR-β和RAR-γ。这些受体在不同的细胞类型和发育阶段有差异表达，表明它们可能调节不同的基因组。我们已经确定了一种具有选择性RAR-α拮抗剂特征的合成类维生素A。这种拮抗剂抵消RA对HL-60细胞分化和B淋巴细胞多克隆活化的影响。除了其潜在的实际意义，这种和其他特定的拮抗剂将是有用的解剖RAR系统，并分配给一个给定的受体的许多RA调节的功能。
Retinoic acid (RA) exerts its pleiotropic effects on cell growth and differentiation through the activation of a family of transcription factors-the RA receptors (RARs). Three subtypes of these receptors exist, RAR-alpha, RAR-beta, and RAR-gamma. The receptors are differentially expressed in different cell types and stages of development, suggesting that they may regulate different sets of genes. We have identified a synthetic retinoid with the characteristics of a selective RAR-alpha antagonist. This antagonist counteracts RA effects on HL-60 cell differentiation and on B-lymphocyte polyclonal activation. Beyond its potential practical relevance, this and other specific antagonists will be useful to dissect the RAR system and to assign to one given receptor each of the many RA-regulated functions.