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Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules and allow selective protein degradation by addressing the natural ubiquitin proteasome system. As this new strategy of chemically induced protein degradation can serve as a biological tool and provides new possibilities for drug discovery, it has been applied to a variety of targets including (nuclear) receptors, kinases, and epigenetic proteins. A lot of PROTACs have already been designed in the field of epigenetics, and their synthesis and characterization highly contributed to structural optimization and improved mechanistic understanding of these molecules. In this review, we will discuss and summarize recent advances in PROTAC discovery with focus on epigenetic targets. Copyright © 2020 The Authors. Published by Elsevier Ltd.. All rights reserved.


Anja Vogelmann, Dina Robaa, Wolfgang Sippl, Manfred Jung. Proteolysis targeting chimeras (PROTACs) for epigenetics research. Current opinion in chemical biology. 2020 Aug;57:8-16

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PMID: 32146413

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