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Pleased to share our story on Structure-Guided Design of a “Bump-and-Hole” Bromodomain-Based #Degradation Tag: BRD4-BD1-L94V #BromoTAG
We combine it with #dTAG to show simultaneous protein depletion!
@DrXiongY @kdonovan1008 @Nicky_eleuteri @fischerlab1
pubs.acs.org/doi/10.1021/ac…
XY-06-007 is a structure based designed CRBN degrader, which binds to BRD4 BD1 L94V and has limited affinity to BRD4 BD1.
Reduced binding to BRD4 BD1 translates to selective degradation of the L94V mutant in a GFP-fusion mCherry reporter line.
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