IDENTIFICATION OF SYNTHETIC RETINOIDS WITH SELECTIVITY FOR HUMAN NUCLEAR RETINOIC ACID RECEPTOR-GAMMA
IDENTIFICATION OF SYNTHETIC RETINOIDS WITH SELECTIVITY FOR HUMAN NUCLEAR RETINOIC ACID RECEPTOR-GAMMA
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DOI：
10.1016/0006-291x(92)90842-9
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发表时间：
1992-07-31
影响因子：
3.1
通讯作者：
SHROOT, B
中科院分区：
文献类型：
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作者：
BERNARD, BA;BERNARDON, JM;SHROOT, B
类视黄醇对基因调控的作用是由三种不同的核视黄酸受体 (RAR) 亚型（RAR α、β 和 γ）介导的。由于 RARγ 主要在成人皮肤中表达，因此该亚型的特定配体可以（i）代表评估 RARγ 在皮肤中的生物学作用的有价值的工具，并且（ii）为治疗实体提供更高的治疗指数和更低的致畸风险。通过体外结合研究和功能反式激活测定，我们鉴定了三种具有高 RARγ 选择性的化合物。
The action of retinoids on gene regulation is mediated by three distinct nuclear retinoic acid receptor (RAR) subtypes called RAR α, β and γ. Since RARγ is predominantly expressed in adult skin, specific ligands for this subtype could (i) represent valuable tools to evaluate the biological role of RARγ in skin and(ii) provide therapeutic entities with a higher therapeutic index at lower teratogenic risk. Using in vitro binding studies and a functional transactivation assay, we have identified three compounds with high RARγ selectivity.