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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
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Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library
Peng Teng1, Xiaolei Zhang, Haifan Wu
1Department of Chemistry, University of South Florida, 4202 E. Fowler Ave, Tampa, FL 33620, USA. jianfengcai@usf.edu.
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.

