Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance

Abstract To identify approaches to target DNA repair vulnerabilities in cancer, we discovered nanomolar potent, selective, low molecular weight (MW), allosteric inhibitors of the polymerase function of DNA polymerase Polθ, including ART558. ART558 inhibits the major Polθ-mediated DNA repair process,... View More