David E. Heppner

In Pursuit of Enduring Inactivation: A Perspective on the Development and Study of Irreversible-Covalent Inhibitors

Abstract Molecules that form irreversible covalent bonds with their targets are a mainstay of drug discovery and chemical biology research. Their ability to permanently inactivate an enzyme target provides a mechanism with significant potential to modulate disease phenotypes. Thi...

A Structural Perspective on Non-covalent Targeting of Conserved Polar Residues in Protein Kinases

Abstract All protein kinases contain conserved amino acid residues that bind the ATP substrate molecule and promote catalysis. As an intensely pursued drug target class, kinase inhibitor development is often streamlined by the utilization of three-dimensional structural data and...