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FUNCTIONAL ANTAGONISM BETWEEN PROTO-ONCOPROTEIN c-JUN AND HORMONE RECEPTORS

机译：原癌蛋白c-Jun与激素受体之间的功能拮抗作用

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摘要

It was demonstrated that hormone receptors and transcription factor Jun / AP-1 repress each other by a mechanism independent of DNA binding. For example, the AP-1 overexpression suppresses activation induced by a gene carrying a functional glucocorticoid response element glucocorticoid. Conversely, it was demonstrated that the glucocorticoid represses gene transcription activation regulated by promoters which contain AP-1 binding site. In addition, the invention relates to methods of selecting compounds useful in the treatment of proliferating cells in an uncontrolled manner, said compounds being capable of interrupting AP-1 function, but they show no ability to promote the activation transcription of hormone-responsive genes.

机译：结果表明，激素受体和转录因子Jun / AP-1通过独立于DNA结合的机制相互抑制。例如，AP-1过表达抑制了由携带功能性糖皮质激素应答元件糖皮质激素的基因诱导的激活。相反，证明了糖皮质激素抑制了由含有AP-1结合位点的启动子调节的基因转录激活。另外，本发明涉及选择以不受控制的方式用于治疗增殖细胞的化合物的方法，所述化合物能够中断AP-1功能，但是它们没有显示出促进激素应答基因的激活转录的能力。

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公开/公告号EP0552202A1

专利类型
公开/公告日1993-07-28

原文格式PDF
申请/专利权人 THE SALK INSTITUTE FOR BIOLOGICAL STUDIES;
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申请/专利号EP19910917435
发明设计人 EVANS RONALD M.;SCHULE ROLAND;
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申请日1991-09-20
分类号A61K38/00;A61K38/22;C07J1/00;C12Q1/68;G01N33/566;G01N33/574;G01N33/68;G01N33/74;
国家 EP
入库时间 2022-08-22 05:05:21

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