Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
13 Jul 2023
13 Jul 2023
Historique:
received:
12
04
2023
accepted:
31
05
2023
pmc-release:
13
07
2024
medline:
19
7
2023
pubmed:
19
7
2023
entrez:
19
7
2023
Statut:
epublish
Résumé
In this study, we describe the rapid identification of potent binders for the WD40 repeat domain (WDR) of DCAF1. This was achieved by two rounds of iterative focused screening of a small set of compounds selected on the basis of internal WDR domain knowledge followed by hit expansion. Subsequent structure-based design led to nanomolar potency binders with a clear exit vector enabling DCAF1-based bifunctional degrader exploration.
Identifiants
pubmed: 37465299
doi: 10.1021/acsmedchemlett.3c00104
pmc: PMC10350940
doi:
Types de publication
Journal Article
Langues
eng
Pagination
949-954Informations de copyright
© 2023 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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