Discovery of RP-37 analogues as potent, selective irreversible inhibitors targeting DNA polymerase theta (POLθ)
{{output}}
DNA polymerase theta (POLθ) is a promising synthetic lethal target for BRCA-deficient cancers, while reversible POLθ-pol inhibitors exhibit limited cellular efficacy. Here, we report the structure-guided discovery of RP-37 analogue B2 as a potent and selecti... ...
