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2017 ; 8
(24
): 39143-39153
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Proton pump inhibitor ilaprazole suppresses cancer growth by targeting
T-cell-originated protein kinase
#MMPMID28388576
Zheng M
; Luan S
; Gao S
; Cheng L
; Hao B
; Li J
; Chen Y
; Hou X
; Chen L
; Li H
Oncotarget
2017[Jun]; 8
(24
): 39143-39153
PMID28388576
show ga
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.