期刊
MOLECULES
卷 26, 期 13, 页码 -出版社
MDPI
DOI: 10.3390/molecules26133915
关键词
bradykinin receptor inhibitor; hepatocellular carcinoma; apoptosis; bradykinin B1 receptor; ERK signaling pathway
资金
- Natural Science Foundation of Jilin Province of China [20180101250 JC]
- 13th Five-Year Science and Technology Project of Jilin Provincial Department of Education [JJKH20180178 KJ]
The novel BK receptor inhibitors J051-71 and J051-105 were found to reduce the viability of liver cancer cells and inhibit colony formation, possibly by inhibiting the ERK pathway. These inhibitors also reversed the cell proliferation induced by BK by downregulating B1 receptor expression, suggesting a potential target for HCC therapy.
Hepatocellular carcinoma (HCC) is the fifth most common cancer worldwide. Studies have shown that bradykinin (BK) is highly expressed in liver cancer. We designed the novel BK receptor inhibitors J051-71 and J051-105, which reduced the viability of liver cancer cells and inhibited the formation of cancer cell colonies. J051-71 and J051-105 reduced cell proliferation and induced apoptosis in HepG2 and BEL-7402 cells, which may be due to the inhibition of the extracellular regulated protein kinase (ERK) signaling pathway. In addition, these BK receptor inhibitors reversed the cell proliferation induced by BK in HepG2 and BEL-7402 cells by downregulating B1 receptor expression. Inhibiting B1 receptor expression decreased the protein levels of p-ERK and reduced the malignant progression of HCC, providing a potential target for HCC therapy.
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