Journal
JOURNAL OF BIOCHEMISTRY
Volume -, Issue -, Pages -Publisher
OXFORD UNIV PRESS
DOI: 10.1093/jb/mvac041
Keywords
PROTACs; proteasome; SNIPERs; targeted protein degradation; ubiquitin
Categories
Funding
- Japan Society for the Promotion of Science
- Ministry of Education, Culture, Sports, Science and Technology (JSPS/MEXT KAKENHI) [JP18H05502, JP21H02777]
- Princess Takamatsu Cancer Research Fund
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Targeted protein degradation is a novel approach for drug discovery and basic research, involving the induction of ubiquitination and proteasomal degradation of target proteins. Various types of degrader molecules have been developed, allowing the rational development of novel degraders for specific proteins of interest.
Targeted protein degradation attracts attention as a novel modality for drug discovery, as well as for basic research. Various types of degrader molecules have been developed so far, which include proteolysis-targeting chimaeras (PROTACs) and specific and nongenetic IAP-dependent protein erasers (SNIPERs), E3 modulators, hydrophobic tagging molecules, IAP antagonists and deubiquitylase inhibitors. PROTACs and SNIPERs are chimeric degrader molecules consisting of a target ligand linked to another ligand that binds to an E3 ubiquitin ligase. In the cells, they recruit an E3 ligase to the target protein, thereby inducing ubiquitylation and proteasomal degradation of the target protein. Because of their modular structure, novel PROTACs and SNIPERs targeting proteins of your interest can be rationally developed by substituting target ligands. In this article, various compounds capable of inducing protein degradation were overviewed, including SNIPER compounds developed in our laboratory.
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