MyJournals Home  

RSS FeedsMolecules, Vol. 27, Pages 6515: Discovery of E3 Ligase Ligands for Target Protein Degradation (Molecules)

 
 

2 october 2022 09:42:43

 
Molecules, Vol. 27, Pages 6515: Discovery of E3 Ligase Ligands for Target Protein Degradation (Molecules)
 


Target protein degradation has emerged as a promising strategy for the discovery of novel therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a cellular ubiquitin-dependent proteolysis system for the efficient degradation of a protein of interest. PROTAC consists of a target protein ligand and an E3 ligase ligand so that it enables the target protein degradation owing to the induced proximity with ubiquitin ligases. Although a great number of PROTACs has been developed so far using previously reported ligands of proteins for their degradation, E3 ligase ligands have been mostly limited to either CRBN or VHL ligands. Those PROTACs showed their limitation due to the cell type specific expression of E3 ligases and recently reported resistance toward PROTACs with CRBN ligands or VHL ligands. To overcome these hurdles, the discovery of various E3 ligase ligands has been spotlighted to improve the current PROTAC technology. This review focuses on currently reported E3 ligase ligands and their application in the development of PROTACs.


 
68 viewsCategory: Biochemistry, Chemistry, Molecular Biology
 
Molecules, Vol. 27, Pages 6513: Essential Roles of Peroxiredoxin IV in Inflammation and Cancer (Molecules)
Molecules, Vol. 27, Pages 6514: Utilization of a Novel Immunofluorescence Instrument Prototype for the Determination of the Herbicide Glyphosate (Molecules)
 
 
blog comments powered by Disqus


MyJournals.org
The latest issues of all your favorite science journals on one page

Username:
Password:

Register | Retrieve

Search:

Molecular Biology


Copyright © 2008 - 2022 Indigonet Services B.V.. Contact: Tim Hulsen. Read here our privacy notice.
Other websites of Indigonet Services B.V.: Nieuws Vacatures News Tweets Nachrichten