Open access
Oct 2026
Integrating Fragment Screening and Covalent Chemistry to Drug DNA-Binding Proteins: RAD52 as a Case Study.
Protein-DNA interfaces are central to genome maintenance but remain challenging targets for small-molecule discovery because they are often broad, polar, solvent-exposed, and lack classical druggable pockets. Here, we establish a structure-guided strategy to chemically target such interfaces by combining the fragment-b...
Nicolas Bocquet, Alessandro Potenza, Jason Clochard et al.
· Journal of the American Chem... · 0 citations