Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs.
E3 modulator
PROTAC
SNIPER
proteasome
protein degradation
ubiquitin
Journal
Frontiers in chemistry
ISSN: 2296-2646
Titre abrégé: Front Chem
Pays: Switzerland
ID NLM: 101627988
Informations de publication
Date de publication:
2019
2019
Historique:
received:
20
09
2019
accepted:
21
11
2019
entrez:
11
1
2020
pubmed:
11
1
2020
medline:
11
1
2020
Statut:
epublish
Résumé
Technologies that induce targeted protein degradation by small molecules have been developed recently. Chimeric small molecules such as Proteolysis Targeting Chimeras (PROTACs) and Specific and Non-genetic IAP-dependent Protein Erasers (SNIPERs), and E3 modulators such as thalidomides, hijack the cellular machinery for ubiquitylation, and the ubiquitylated proteins are subjected to proteasomal degradation. This has motivated drug development in industry and academia because "undruggable targets" can now be degraded by targeted protein degradation.
Identifiants
pubmed: 31921772
doi: 10.3389/fchem.2019.00849
pmc: PMC6914816
doi:
Types de publication
Journal Article
Review
Langues
eng
Pagination
849Informations de copyright
Copyright © 2019 Naito, Ohoka, Shibata and Tsukumo.
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