PARP1 inhibitors regulate PARP1 structure independent of DNA, reducing binding affinity for single strand breaks
Mark Pailing, Lotte van Beek, Taianá Maia de Oliveira, Maria M. Flocco, Bart W. Hoogenboom
This study shows PARP inhibitors reduce PARP1's DNA binding affinity by causing conformational changes independent of DNA, explaining similar cellular toxicities despite varying trapping potencies.
bioRxiv · Aug 30, 2025 · PreprintBiophysics