从一个γ-氨基酸肽基于珠的组合文库中鉴定破坏STAT3与DNA相互作用的新型抑制剂。
Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library.
作者信息
Teng Peng, Zhang Xiaolei, Wu Haifan, Qiao Qiao, Sebti Said M, Cai Jianfeng
机构信息
Department of Chemistry, University of South Florida, 4202 E. Fowler Ave, Tampa, FL 33620, USA.
出版信息
Chem Commun (Camb). 2014 Aug 14;50(63):8739-42. doi: 10.1039/c4cc03909b. Epub 2014 Jun 25.
Abstract
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.
摘要
从基于γ-氨基酸肽的单珠单化合物（OBOC）组合文库中，我们鉴定出了能够选择性抑制STAT3与DNA相互作用并抑制完整细胞中STAT3靶基因表达水平的γ-氨基酸肽。我们的结果表明，除了SH2结构域之外，STAT3的DNA结合结构域也可作为新一代抗癌治疗药物开发的靶点。
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