Discover and read the best of Twitter Threads about #PROTAC
Most recents (3)
The #AACR23 abstracts will be accessible from here (not all sessions populated yet at the time of this tweet)
abstractsonline.com/pp8/#!/10828/
abstractsonline.com/pp8/#!/10828/
"new drugs on the horizon":
ND03 - Discovery of ARV-766, an androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer $ARVN #PROTAC
abstractsonline.com/pp8/#!/10828/p…
ND03 - Discovery of ARV-766, an androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer $ARVN #PROTAC
abstractsonline.com/pp8/#!/10828/p…
ND01 - ABBV-319: A first-in-class Glucocorticoid Receptor Modulator (GRM) agonist #ADC for the treatment of B-cell malignancies $ABBV
abstractsonline.com/pp8/#!/10828/p…
abstractsonline.com/pp8/#!/10828/p…
On @biorxivpreprint we report a direct TR-FRET-based protein quantification strategy (<1 h from lysis➡️read) in unmodified cell lines. If you're into PROTACs, and you hate running Westerns, check it out! Mini-thread: (1/n)
biorxiv.org/content/10.110…
biorxiv.org/content/10.110…
Two birds with one stone: using clever biochemistry principles and a single POI-targeting antibody, we can rapidly & quantitatively measure both endogenous target engagement and protein levels in whole cell extracts, here exemplified for BRD4 (2/n) 
A conventional blood-sweat-and-tears Western blot takes the average scientist 2 days. With our strategy, we initially optimized the assay in a 24-well plate format. The readout takes <1 h. Comparing BRD4 levels measured by our platform to Western blot were nearly identical (3/n)
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…
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.
