ART6043 (Polθ-IN-7) is an orally active, selective allosteric DNA polymerase θ ( Polθ ) inhibitor with an IC 50 of 1.3 nM. ART6043 blocks microhomology-mediated end joining (MMEJ) by inhibiting the polymerase function of Polθ . ART6043 suppresses the survival of homologous recombination-deficient (HRD) cells and enhances the antitumor effects of PARP inhibitors. ART6043 can be used in studies of HRD tumors, including BRCA1-mutant triple-negative breast cancer , BRCA2-deficient colorectal cancer , RAD51C-deficient gastric cancer , and others .
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