Targeting a Pleckstrin Homology Domain with a Lysine-Reactive Cova-lent Binder
Rebekah M. West, Radu Costin Bizga Nicolescu, P. Brear, James Mark Wagstaff, Beata K. Blaszczyk, Tomáš Deingruber, Matthew G. Sanders, Francisco Javier Pérez-Areales, David R. Spring, Marko Hyvönen
The paper identifies a covalent binder targeting a lysine in the PIP3 binding site of BTK's PH domain, offering a novel approach to inhibit BTK beyond traditional ATP site targeting.
Journal of Medicinal Chemistry · May 14, 2026Peer-reviewedBiochemistry