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Oxopiperazine helix mimetics for control of Hypoxia-Inducible gene expression

机译:Oxopiperazine螺旋模拟物控制缺氧诱导型基因表达

摘要

The present invention relates to oxopiperazines that mimic helix αB of the C-terminal transactivation domain of HIF1α. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1a with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).
机译:本发明涉及模拟HIF1α的C末端反式激活结构域的螺旋αB的氧杂哌嗪。还公开了包含这些氧代哌嗪的药物组合物和使用这些氧代哌嗪的方法(例如,减少基因转录,治疗或预防由HIF1a与CREB结合蛋白和/或p300相互作用介导的疾病,减少或防止组织中的血管生成,诱导凋亡,并降低细胞存活和/或增殖)。

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