Happy to present our latest paper with @pottslab & @Amgen in @J_A_C_S by co-first authors @C_M_Zammit & Cory Nadel on the discovery of a direct-acting covalent destabilizing degrader of AR and the undruggable truncation variant of AR, AR-V7, in androgen-independent prostate cancer cells that acts through targeting an IDR C125. Thanks also to @TheMarkFdn! https://t.co/2sUmRmJdax
Kudos to @VividionRx for finding a small molecule activator of the KEAP1-CUL3 interaction. Really revealing that this interaction turned out to be rate-limiting for NRF2 degradation. Congratulations!
https://t.co/eQBbzh3BPE
Vividion Continues to Teach Covalent Compounds New Tricks | https://t.co/hcTUn8y5yB
At the recent ACS Fall 2024 meeting, the structure and discovery story of Vividion's clinical oral covalent activator of KEAP1 were disclosed.
New MLKL degraders. Will note that the covalent handle abrogates potential turnover - these become stoichiometric. But still seem to degrade reasonably.
https://t.co/KU9bjQtxtu
A new paper from Dylan Dieters-Castator describing the workflow development of a sensitive and robust N-Glycoproteomics workflow to enrich cell surface proteins. Congrats Dylan! https://t.co/BnlzTSGvmH
A designed peptide selectively reacts with a single lysine residue on Nck, disrupts phase-separated signaling coacervates, shuts down an intracellular signal, & inhibits E. coli infection
NEW #ASAP by Jiang Xia, Chunjian Wu & team #CUHK
Read it here: https://t.co/PQPvGKG967
$XBI has just witnessed the best 2-month stretch EVER for the sector
It has seen 8 consecutive weeks of gains, up +14% in Nov and +18% more in Dec, or 39% off the Oct lows.
Fed rates, M&A boom, good data, cash recycling - all conspiring.
thx to Jack Bannister at Leerink
Using a Function-First “Scout Fragment”-Based Approach to Develop Allosteric Covalent Inhibitors of Conformationally Dynamic Helicase Mechanoenzymes | Journal of the American Chemical Society https://t.co/soow7jqfxS