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YAP1 inhibitors that target the interaction of YAP1 with Oct4

机译:靶向YAP1与Oct4相互作用的YAP1抑制剂

摘要

Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit stemness. Disclosed are compounds that affect the Yap1:Oct4 interaction.
机译:转录共激活因子YAP1与转录因子Oct4的结合可诱导Sox2,Sox2是非小细胞肺癌干细胞自我更新所必需的转录因子。 YAP1的WW域与Oct4的PPxY基序结合以诱导Sox2。递送对应于WW结构域的肽可以防止Sox2的诱导和茎干。同样,PPxY基序的肽和模拟物将能够抑制茎干。公开了影响Yap1:Oct4相互作用的化合物。

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