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METHOD FOR THE IDENTIFICATION AND CHARACTERIZATION OF NUCLEAR RECEPTOR LIGANDS

机译:核受体配体的鉴定和表征方法

摘要

The present invention is directed to a methodology to study the effect of ligands that can modulate functions of nuclear receptors, and specifically, their interaction with specific DNA or other transcription factors. These receptors play a major role in the cascade of inter and intracellular physiological and biochemical events. They generally have a modular construction which enables them to recognize and bind to certain DNA sequences, or binding elements, such as hormone response elements. Various ligands, such as hormones, affect this interaction. In accordance with the methodology presented herein, measurements of such interactions are taken in real time and kinetic pattern. This allows the user to identify and to characterize ligands that are able to affect a receptor's interaction with its binding element. Hence, the present invention provides a useful tool for the elucidation, and development of ligands that affect transcription of target genes, either directly or indirectly.
机译:本发明涉及一种研究配体的作用的方法,所述配体可以调节核受体的功能,特别是其与特定DNA或其他转录因子的相互作用。这些受体在细胞间和细胞内生理和生化事件的级联中起主要作用。它们通常具有模块化的结构,使它们能够识别并结合到某些DNA序列或结合元件,例如激素反应元件。各种配体(例如激素)会影响这种相互作用。根据本文提出的方法,以实时和动态模式进行这种相互作用的测量。这使用户能够鉴定和表征能够影响受体与其结合元件相互作用的配体。因此,本发明提供了用于阐明和开发直接或间接影响靶基因转录的配体的有用工具。

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