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Using a Function-First “Scout Fragment”-Based Approach to Develop Allosteric Covalent Inhibitors of Conformationally Dynamic Helicase Mechanoenzymes | Journal of the American Chemical Society pubs.acs.org/doi/10.1021/ja…

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: go.acs.org/7By

$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

Design and Evaluation of PROTACs Targeting Acyl Protein Thioesterase 1 - Carvalho - ChemBioChem - Wiley Online Library …mistry-europe.onlinelibrary.wiley.com/doi/10.1002/cb…

biorxiv.org/content/10.110…

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! pubs.acs.org/doi/10.1021/ac…

Watch CEO Matt Gline reflect on Telavant #success, Immunovant's FcRn program, and our best-in-class pipeline with @BiotechTVHQ and Brad Loncar! #biotech #innovation

Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs | Journal of Medicinal Chemistry pubs.acs.org/doi/10.1021/ac…

Redirecting the pioneering function of FOXA1 with covalent small molecules biorxiv.org/cgi/content/sh… #bioRxiv

Reversible Covalent Inhibition─Desired Covalent Adduct Formation by Mass Action dlvr.it/T542nb

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Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches - Covalent Drug Discovery is just warming up. pubmed.ncbi.nlm.nih.gov/38728572/?utm_…

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Come join our team of talented drug hunters to discover the next generation of #covalent #therapeutics boards.greenhouse.io/covant/jobs/61…

Aminomethyl Salicylaldehydes Lock onto a Surface Lysine by Forming an Extended Intramolecular Hydrogen Bond Network dlvr.it/TCP1hT

New MLKL degraders. Will note that the covalent handle abrogates potential turnover - these become stoichiometric. But still seem to degrade reasonably. pubs.acs.org/doi/10.1021/ac…

Vividion Continues to Teach Covalent Compounds New Tricks | drughunters.com/47TX5jU At the recent ACS Fall 2024 meeting, the structure and discovery story of Vividion's clinical oral covalent activator of KEAP1 were disclosed.

New bioRxiv from Gray lab Sarafan ChEM-H on covalent degraders based on SNaR chemistry to exploits DCAF16/11. biorxiv.org/content/10.110…

Kudos to Vividion Therapeutics 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! biorxiv.org/content/10.110…

Happy to present our latest paper with Ryan Potts & Amgen 🧪🔬🧬 in J. Am. Chem. Soc. by co-first authors Charlotte 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