Shruti Lal, Neil E Bhola, Bee-Chun Sun, Yuping Chen, Tom Huang, Vivian Morton, Kevin X Chen, Shanghua Xia, Haoyu Zhang, Nehal S Parikh, Qiuping Ye, O Petter Veiby, David I Bellovin, Yuhua Ji
UNLABELLED: DNA-dependent protein kinase (DNA-PK), a driver of the non-homologous end-joining (NHEJ) DNA damage response pathway, plays an instrumental role in repairing double-strand breaks (DSB) induced by DNA-damaging poisons. We evaluate ZL-2201, an orally bioavailable, highly potent, and selective pharmacologic inhibitor of DNA-PK activity, for the treatment of human cancerous malignancies. ZL-2201 demonstrated greater selectivity for DNA-PK and effectively inhibited DNA-PK autophosphorylation in a concentration- and time-dependent manner...
September 2023: Cancer Res Commun