Novel role of apatinib as a multi-target RTK inhibitor in the direct suppression of hepatocellular carcinoma cells

Biochimica Et Biophysica Acta. Molecular Basis of Disease
Xiaojin LiJian Huang

Abstract

Although apatinib has been demonstrated with potential antitumor activity in multiple solid tumors, the underlying mechanism of apatinib for the treatment of hepatocellular carcinoma (HCC) remains unclear. In the present study, we explored if there are any direct suppression effects of apatinib on HCC cells and its relevant targets. We investigated the effect of apatinib on viability of five HCC cell lines and an intrahepatic cholangiocarcinoma cell line, and colony formation, apoptosis and migration of representative HCC cells in vitro; and HCC progression in a xenograft mouse model. Using a phospho-receptor tyrosine kinase pathway array with 49 different tyrosine kinases, we screened and verified the tyrosine kinase targets involved in apatinib response. Apatinib treatment significantly inhibited HCC cell viability, proliferation, colony formation, and migration, and enhanced cell apoptosis in a concentration-dependent manner (p < 0.05). Furthermore, apatinib showed a favorable anti-tumor growth effect (71% of inhibition ratio, p < 0.05) in an established human HCC xenograft mice model with good safety. RTK pathway arrays and western blots analysis demonstrated that apatinib significantly downregulated the phosphorylation lev...Continue Reading

Citations

Aug 18, 2018·Plastic and Reconstructive Surgery·Leonidas Pavlidis
Dec 18, 2018·Endocrine Connections·Shan WuZai Wang
Jul 2, 2020·The Journal of Pharmacy and Pharmacology·Xiao-Dan ZhangJian-Chang Qian
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Apr 28, 2020·World Journal of Clinical Cases·Jun-Hui GuoHai-Rui Duan
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May 14, 2021·Frontiers in Oncology·Hui XiaZhao Gong
Sep 23, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Pengpeng LiuQuanyan Liu

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