Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field.

ABSTRACT: 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.

SUBMITTER: Vulpetti A 

PROVIDER: S-EPMC10350940 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature