Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library.
Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library.
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从 γ-AApeptide OBOC 组合库中鉴定破坏 STAT3-DNA 相互作用的新型抑制剂。
DOI：
10.1039/c4cc03909b
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发表时间：
2014
期刊：
影响因子：
--
通讯作者：
Cai,Jianfeng
中科院分区：
文献类型：
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作者：
Teng,Peng;Zhang,Xiaolei;Wu,Haifan;Qiao,Qiao;Sebti,SaidM;Cai,Jianfeng
从一个基于γ-A肽的一珠一化合物组合文库中，我们发现γ-A肽可以选择性地抑制STAT3DNA相互作用，并抑制完整细胞中STAT3靶基因的表达水平。我们的结果表明，除了SH2结构域之外，STAT3的DNA结合结构域也是开发新一代抗癌药物的靶点。
From a γ-AApeptide-based one-bead-one-compound (OBOC) combinatorial library, we identified γ-AApeptides that can selectively inhibit STAT3–DNA interaction and suppress the expression levels of STAT3 target genes in intact cells. Our results demonstrate that in addition to the SH2 domain, the DNA binding domain of STAT3 is targetable for the development of a new generation of anti-cancer therapeutics.