Targeting Aurora B kinase with Tanshinone IIA suppresses tumor growth and overcomes radioresistance

Abstract Aurora B kinase is aberrantly overexpressed in various tumors and shown to be a promising target for anti-cancer therapy. In human oral squamous cell carcinoma (OSCC), the high protein level of required maintaining malignant phenotypes, including vitro growth, colony formation, vivo tumor development. By molecular modeling screening 74 commercially available natural products, we identified that Tanshinone IIA (Tan IIA), as potential inhibitor. The silico docking study indicates Tan docks into ATP-binding pocket B, which further confirmed by assay, ex pull-down, ATP competitive binding assay. exhibited significant anti-tumor effect on OSCC cells both vivo, reduction histone H3 phosphorylation, induction G2/M cycle arrest, increase population polyploid cells, promotion apoptosis. mouse model revealed delayed growth cells. alone or combination with radiation overcame radioresistance xenograft tumors. Taken together, our data indicate an inhibitor therapeutic potentials cancer treatment.