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

Fuchun Xie, Qiuhua Fan, Bingbing X. Li, Xiangshu Xiao

Research output: Contribution to journalArticle

2 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)11423-11429
Number of pages7
JournalJournal of Medicinal Chemistry
Volume62
Issue number24
DOIs
StatePublished - Dec 26 2019

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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