title: Developments of DNA-dependent Protein Kinase Inhibitors as Anticancer Agents.
abstract: 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 (DNA-PK), 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).
authors.forename: Chen-Chen
authors.initials: CC
authors.lastname: Ma
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.forename: Ren-Zhong
authors.initials: RZ
authors.lastname: Wan
authors.affiliation: . liuzhaop@sdu.edu.cn.
authors.forename: Zhao-Peng
authors.initials: ZP
authors.lastname: Liu