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 - as a potent CREB inhibitor. Herein, we designed an ester prodrug of - through a long-range ,-acyl transfer reaction for improved aqueous solubility. Unexpectedly, we discovered a small molecule (-) that can potentiate the CREB inhibitory activity of - although - alone does not inhibit CREB.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10355536 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.9b01207 | DOI Listing |
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