4.7 Article

Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library

Journal

CHEMICAL COMMUNICATIONS
Volume 50, Issue 63, Pages 8739-8742

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c4cc03909b

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Funding

  1. Elsa Pardee Foundation
  2. Florida Bankhead-Coley program
  3. NIH [RO1 CA140681-05]

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From a gamma-AApeptide-based one-bead-one-compound (OBOC) combinatorial library, we identified gamma-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.

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