Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field
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Date
2023-07-13
Publication Type
Journal Article
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Abstract
In this study, we describe the rapid identification ofpotent bindersfor the WD40 repeat domain (WDR) of DCAF1. This was achieved by tworounds of iterative focused screening of a small set of compoundsselected on the basis of internal WDR domain knowledge followed byhit expansion. Subsequent structure-based design led to nanomolarpotency binders with a clear exit vector enabling DCAF1-based bifunctionaldegrader exploration.
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published
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Volume
14 (7)
Pages / Article No.
949 - 954
Publisher
American Chemical Society
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Subject
Virtual screening; Structure-based design; Biophysics; DCAF1; E3 ligase; TPD