2. Academic Validation
  3. Proteolysis targeting chimeras (PROTACs) for epigenetics research

Proteolysis targeting chimeras (PROTACs) for epigenetics research

  • Curr Opin Chem Biol. 2020 Aug;57:8-16. doi: 10.1016/j.cbpa.2020.01.010.
Anja Vogelmann 1,  Dina Robaa 2,  Wolfgang Sippl 2,  Manfred Jung 3
Affiliations

Affiliations

  • 1 Institute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, Freiburg, 79104, Germany.
  • 2 Institute of Pharmaceutical Chemistry, Martin-Luther University of Halle-Wittenberg, Wolfgang-Langenbeckstraße 4, Halle/Saale, 06120, Germany.
  • 3 Institute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, Freiburg, 79104, Germany; CIBSS - Centre for Integrative Biological Signalling Studies, University of Freiburg, Schänzlestraße 18, Freiburg, 79104, Germany. Electronic address: [email protected].
PMID: 32146413 DOI: 10.1016/j.cbpa.2020.01.010
Abstract

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.

Keywords

Drug discovery; Epigenetics; PROTACs; Protein degradation.

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