首页> 外国专利> INHIBITING INTERACTION BETWEEN HIF-1A AND P300/CBP WITH HYDROGEN BOND SURROGATE-BASED HELICES

INHIBITING INTERACTION BETWEEN HIF-1A AND P300/CBP WITH HYDROGEN BOND SURROGATE-BASED HELICES

机译:抑制HIF-1A和P300 / CBP与基于氢键的基于替代物的HEL头之间的相互作用

摘要

The present invention relates to peptides having one or more stable, internally constrained a-helices, and that include a sequence that mimics at least a portion of the C-terminal transactivation domain of HIF-la. Also disclosed are pharmaceutical compositions containing these peptides and methods of using these peptides, for example to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF-la with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, decrease cell survival and/or proliferation, and identify potential ligands of CREB-binding protein and/or p300.
机译:本发明涉及具有一个或多个稳定的,内部受约束的α-螺旋的肽,其包括模拟HIF-1α的C端反式激活结构域的至少一部分的序列。还公开了包含这些肽的药物组合物和使用这些肽的方法,例如减少基因转录,治疗或预防由HIF-1α与CREB结合蛋白和/或p300相互作用介导的疾病,减少或预防组织中的血管生成,诱导细胞凋亡,降低细胞存活和/或增殖,并鉴定CREB结合蛋白和/或p300的潜在配体。

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