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Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins

5 Jun 2023

Abstract excerpt

The histone acetyltransferase CREB-binding protein (CBP) and its paralogue p300 protein are key transcriptional coactivators and attractive cancer therapeutic targets. We describe herein our design, synthesis, and extensive evaluation of exceptionally potent PROTAC degraders of CBP/p300, exemplified by JET-209 ( 24 ). This compound, JET-209, achieved a half-maximal degradation (DC 50 ) value of 0.05 nM for CBP...

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PMID: 37276143
DOI: 10.1021/acs.jmedchem.3c00492

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