Submit Manuscript  

Article Details

Developments of DNA-dependent Protein Kinase Inhibitors as Anticancer Agents

[ Vol. 14 , Issue. 11 ]


Chen-Chen Ma, Hui Li, Ren-Zhong Wan and Zhao-Peng Liu   Pages 884 - 895 ( 12 )


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).


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.


Institute of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P.R. China.

Read Full-Text article