申请人:H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
公开号:US11530182B2
公开(公告)日:2022-12-20
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 sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.
转录共激活因子YAP1与转录因子Oct4结合可诱导Sox2,Sox2是非小细胞肺癌干样细胞自我更新所必需的转录因子。YAP1的WW结构域与Oct4的PPxY基序结合,诱导Sox2。输送与WW结构域相对应的多肽可以阻止Sox2的诱导和干性。同样,PPxY基团的多肽和模拟物也能抑制干性。已公开的化合物会影响 Yap1:Oct4 的相互作用。