ArticleACS medicinal chemistry letters2026
Targeting Histone Acetyltransferases EP300/CBP by Novel Proline-Based PROTAC Degraders.
Article in ACS medicinal chemistry letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
E1A-binding proteins p300 (EP300) and CREB-binding protein (CBP) are two homologous multidomain enzymes that have emerged as promising therapeutic targets in oncology. Recent drug discovery efforts have yielded degraders that target EP300/CBP by engaging either the bromodomain or the histone acetyltransferase (HAT) domain, with the latter potentially leading to preferential or selective degradation of one paralog. Building on a potent proline-based EP300/CBP HAT domain inhibitor, we designed, synthesized, and characterized a series of novel HAT-targeting and cereblon-recruiting proteolysis-targeting chimeras (PROTACs). In particular, compound
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