Repair of DNA double-strand breaks (DSBs) is critical for the maintenance of genome integrity, cell survival,
and prevention tumorigenesis. Three pathways are responsible for the repair of DNA DSBs: homologous recombination
(HR), single strand annealing (SSA) and non-homologous end joining (NHEJ). DNA-dependent Protein Kinase (DNAPK),
the key component of the NHEJ pathway, becomes an important target for cancer therapy. A large number of small
molecules exhibit inhibitory activities against DNA-PK in an ATP-competitive manner. This paper reviews the recent
developments of a diversity of small molecule DNA-PK inhibitors, with emphasis on their structural features, biological
activities, and structure-activity relationships (SARs).
Keywords: Anticancer, anticancer agents, ATP-competitive inhibitors, chemo- and radio-potentiation, DNA-dependent protein
kinase (DNA-PK), DNA double-strand breaks (DSBs), DNA-PK inhibitors, DNA-PK catalytic subunit, PI3K, cytotoxicity,
inhibitory activity, kinase selectivity.
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