首页> 外国专利> IDENTIFICATION AND USE OF SMALL MOLECULES TO MODULATE ESE-1 TRANSCRIPTION FACTOR FUNCTION AND TO TREAT ESE-1 TRANSCRIPTION FACTOR ASSOCIATED DISEASES

IDENTIFICATION AND USE OF SMALL MOLECULES TO MODULATE ESE-1 TRANSCRIPTION FACTOR FUNCTION AND TO TREAT ESE-1 TRANSCRIPTION FACTOR ASSOCIATED DISEASES

机译:鉴定和使用小分子调节ESE-1转录因子功能并治疗ESE-1转录因子相关疾病

摘要

The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor.
机译:本发明涉及鉴定能够调节转录因子功能的小分子候选试剂的方法,使得靶转录因子和/或该靶蛋白下游的蛋白的功能/表达包括使用计算机高通量筛选小分子文库对接候选小分子/试剂,这些小分子/试剂通过药效团内定义的独特转录因子和/或DNA描述符选择性靶向和破坏转录因子-DNA界面的能力,然后测试/评估上述鉴定的候选试剂通过一种或多种体外测定其调节转录因子功能的能力,包括该靶蛋白和/或靶转录因子下游蛋白的表达。

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