Research Papers:

Proton pump inhibitor ilaprazole suppresses cancer growth by targeting T-cell-originated protein kinase

Mengzhu Zheng, Shanshan Luan, Suyu Gao, Li Cheng, Bin Hao, Jiacheng Li, Yao Chen, Xuemei Hou, Lixia Chen and Hua Li _

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Oncotarget. 2017; 8:39143-39153. https://doi.org/10.18632/oncotarget.16609

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Mengzhu Zheng2,*, Shanshan Luan2,*, Suyu Gao1, Li Cheng2, Bin Hao2, Jiacheng Li2, Yao Chen2, Xuemei Hou3, Lixia Chen1 and Hua Li1,2

1School of Traditional Chinese Materia Medica, Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China

2Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China

3Livzon Pharmaceutical Group Inc., Zhuhai 519090, China

*These authors have contributed equally to this work

Correspondence to:

Hua Li, email: [email protected]

Lixia Chen, email: [email protected]

Xuemei Hou, email: [email protected]

Keywords: Ilaprazole, PPI, cancer, drug repurposing, TOPK inhibitor

Received: January 23, 2017     Accepted: March 02, 2017     Published: March 27, 2017


T-cell-originated protein kinase (TOPK) is highly and frequently expressed in various cancer tissues and plays an indispensable role in the mitosis of cancer cells, and therefore, it is an important target for drug treatment of tumor. Ilaprazole was identified to be a potent TOPK inhibitor. The data indicated that ilaprazole inhibited TOPK activities with high affinity and selectivity. In vitro studies showed that ilaprazole inhibited TOPK activities in HCT116, ES-2, A549, SW1990 cancer cells. Moreover, knockdown of TOPK in these cells decreased their sensitivities to ilaprazole. Results of an in vivo study demonstrated that gavage of ilaprazole in HCT116 colon tumor-bearing mice effectively suppressed cancer growth. The TOPK downstream signaling molecule phospho-histone H3 in tumor tissues was also decreased after ilaprazole treatment. Our results suggested that ilaprazole inhibited the cancer growth by targeting TOPK both in vitro and in vivo.

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