Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction.
HEK293 Cells
Humans
Phosphorylation
/ drug effects
Protein Binding
/ drug effects
Proteolysis
/ drug effects
Small Molecule Libraries
/ analysis
Substrate Specificity
/ drug effects
Ubiquitin-Protein Ligases
/ metabolism
Ubiquitination
/ drug effects
beta Catenin
/ metabolism
beta-Transducin Repeat-Containing Proteins
/ metabolism
Journal
Nature communications
ISSN: 2041-1723
Titre abrégé: Nat Commun
Pays: England
ID NLM: 101528555
Informations de publication
Date de publication:
29 03 2019
29 03 2019
Historique:
received:
25
10
2018
accepted:
07
03
2019
entrez:
31
3
2019
pubmed:
31
3
2019
medline:
6
5
2019
Statut:
epublish
Résumé
Protein-protein interactions (PPIs) governing the recognition of substrates by E3 ubiquitin ligases are critical to cellular function. There is significant therapeutic potential in the development of small molecules that modulate these interactions; however, rational design of small molecule enhancers of PPIs remains elusive. Herein, we report the prospective identification and rational design of potent small molecules that enhance the interaction between an oncogenic transcription factor, β-Catenin, and its cognate E3 ligase, SCF
Identifiants
pubmed: 30926793
doi: 10.1038/s41467-019-09358-9
pii: 10.1038/s41467-019-09358-9
pmc: PMC6441019
doi:
Substances chimiques
Small Molecule Libraries
0
beta Catenin
0
beta-Transducin Repeat-Containing Proteins
0
Ubiquitin-Protein Ligases
EC 2.3.2.27
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
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