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Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity

22 Apr 2024

Abstract excerpt

The transcriptional coactivator cAMP response element binding protein (CREB)-binding protein (CBP) and its homologue p300 have emerged as attractive therapeutic targets for human cancers such as acute myeloid leukemia (AML). Herein, we report the design, synthesis, and biological evaluation of a series of cereblon (CRBN)-recruiting CBP/p300 proteolysis targeting chimeras (PROTACs) based on the inhibitor CCS1477....

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PMID: 38649304
DOI: 10.1021/acs.jmedchem.3c02195

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Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor ActivityPMID 38649304Read ↗

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