{"title":"Recent Advances in CBP/EP300 Degraders.","authors":"Leonardo Palaferri, Iván Cheng-Sánchez, Cristina Nevado","doi":"10.2533/chimia.2025.137","DOIUrl":null,"url":null,"abstract":"<p><p>Targeted protein degradation (TPD) has emerged as an innovative therapeutic strategy, offering advantage over traditional approaches rooted in small-molecule inhibitors. Among the various modalities in TPD, proteolysis targeting chimeras (PROTACs) and molecular glue degraders (MGDs) have arisen as leading modalities, distinguished by their ability to induce protein degradation via the ubiquitin-proteasome system (UPS). In recent years, extensive research has focused on developing degraders targeting CREB-binding protein (CBP) and E1A-associated protein (EP300) - two homologous multidomain enzymes critical for enhancer-mediated transcription. This review explores the state of the art in CBP/EP300 degraders, underscoring the significant potential of these synthetic bifunctional compounds as innovative chemical tools and highly promising anticancer agents.</p>","PeriodicalId":9957,"journal":{"name":"Chimia","volume":"79 3","pages":"137-145"},"PeriodicalIF":1.1000,"publicationDate":"2025-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chimia","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.2533/chimia.2025.137","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
Targeted protein degradation (TPD) has emerged as an innovative therapeutic strategy, offering advantage over traditional approaches rooted in small-molecule inhibitors. Among the various modalities in TPD, proteolysis targeting chimeras (PROTACs) and molecular glue degraders (MGDs) have arisen as leading modalities, distinguished by their ability to induce protein degradation via the ubiquitin-proteasome system (UPS). In recent years, extensive research has focused on developing degraders targeting CREB-binding protein (CBP) and E1A-associated protein (EP300) - two homologous multidomain enzymes critical for enhancer-mediated transcription. This review explores the state of the art in CBP/EP300 degraders, underscoring the significant potential of these synthetic bifunctional compounds as innovative chemical tools and highly promising anticancer agents.
期刊介绍：
CHIMIA, a scientific journal for chemistry in the broadest sense covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.
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