BTK dynamics and function are differentially influenced by distinct covalent inhibitor warhead chemistries.
Raji E. Joseph, Robert G. Britton, David Yin-wei Lin, Julien Roche, Jeffrey A. Purslow, D. Bruce Fulton, Poowadon Fukasem, M. Paul Gleeson, Martin J.S. Dyer, Thomas E. Wales, Amy Hamilton Andreotti
This study compares the effects of different warhead chemistries in covalent inhibitors on BTK dynamics and function, showing that 2-butynamide induces conformational heterogeneity and reduced efficacy compared to acrylamide.
bioRxiv · Oct 17, 2026 · PreprintBiochemistry