Proteolysis targeting chimeras (PROTACs) for epigenetics research
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
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Notes
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Current opinion in chemical biology. - 57 (2020) , 8-16, ISSN: 1879-0402
- Event
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Veröffentlichung
- (where)
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Freiburg
- (who)
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Universität
- (when)
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2023
- Creator
- Contributor
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Pharmazeutische und Medizinische Chemie, Arbeitskreis Manfred Jung
- DOI
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10.1016/j.cbpa.2020.01.010
- URN
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urn:nbn:de:bsz:25-freidok-1717031
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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14.08.2025, 10:52 AM CEST
Data provider
This object is provided by:
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Vogelmann, Anja
- Robaa, Dina
- Sippl, Wolfgang
- Jung, Manfred
- Pharmazeutische und Medizinische Chemie, Arbeitskreis Manfred Jung
- Universität
Time of origin
- 2023
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Synthese und Untersuchung von peptidischen Substraten der Histondeacetylasen
Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren
Molecular Modelling Untersuchungen zum Bindungsverhalten von Histamin H2- und H3-Rezeptor-Liganden
HaloTag‐Targeted Sirtuin‐Rearranging Ligand (SirReal) for the Development of Proteolysis‐Targeting Chimeras (PROTACs) against the Lysine Deacetylase Sirtuin 2 (Sirt2) **
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Klinische Erfahrungen mit N1-n-Butylbiguanid in der Behandlung des Diabetes mellitus
Compton-Effekt am Proton im Bereich der ersten Resonanz : (Messung differentieller Wirkungsquerschnitte)
HaloTag‐targeted sirtuin‐rearranging ligand (SirReal) for the development of proteolysis‐targeting chimeras (PROTACs) against the lysine deacetylase sirtuin 2 (Sirt2)
Design, synthesis and biological characterization of histone deacetylase 8 (HDAC8) proteolysis targeting chimeras (PROTACs) with anti-neuroblastoma activity
Epigenetic targets in drug discovery
Carbamates as potential prodrugs and a new warhead for HDAC inhibition
Defined stereoisomers of 2″-amino NAD+ and their activity against human sirtuins and a bacterial (ADP-ribosyl) transferase
Synthese und Untersuchung von peptidischen Substraten der Histondeacetylasen
Design, Synthese und Charakterisierung neuer Sirtuin Inhibitoren
Molecular Modelling Untersuchungen zum Bindungsverhalten von Histamin H2- und H3-Rezeptor-Liganden
HaloTag‐Targeted Sirtuin‐Rearranging Ligand (SirReal) for the Development of Proteolysis‐Targeting Chimeras (PROTACs) against the Lysine Deacetylase Sirtuin 2 (Sirt2) **
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Klinische Erfahrungen mit N1-n-Butylbiguanid in der Behandlung des Diabetes mellitus
Compton-Effekt am Proton im Bereich der ersten Resonanz : (Messung differentieller Wirkungsquerschnitte)
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Carbamates as potential prodrugs and a new warhead for HDAC inhibition