2. Academic Validation
  3. Discovery of a Synergistic Inhibitor of cAMP-Response Element Binding Protein (CREB)-Mediated Gene Transcription with 666- 15

Discovery of a Synergistic Inhibitor of cAMP-Response Element Binding Protein (CREB)-Mediated Gene Transcription with 666- 15

  • J Med Chem. 2019 Dec 26;62(24):11423-11429. doi: 10.1021/acs.jmedchem.9b01207.
Fuchun Xie,  Qiuhua Fan,  Bingbing X Li,  Xiangshu Xiao
PMID: 31765143 DOI: 10.1021/acs.jmedchem.9b01207
Abstract

CREB is a transcription factor implicated in the pathogenesis of multiple cancers. Targeting CREB is a promising strategy to develop potential Cancer therapeutics. Previously, we identified 666-15 as a potent CREB inhibitor. Herein, we designed an ester prodrug of 666-15 through a long-range O,N-acyl transfer reaction for improved aqueous solubility. Unexpectedly, we discovered a small molecule 11 (653-47) that can potentiate the CREB inhibitory activity of 666-15 although 653-47 alone does not inhibit CREB.

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