Key result
BQ-123 inhibits endothelin-1-induced upregulation of tumor-associated proteinases in ovarian carcinoma cells.
Why the study?
Does Endothelin-1 induce production and activation of tumour-associated proteinases in ovarian carcinoma cells?
Does Endothelin-1 induce production and activation of tumour-associated proteinases in ovarian carcinoma cells?
Endothelin-1 promotes the secretion and activation of multiple proteinases in ovarian carcinoma cells via the ET(A) receptor, suggesting a role in tumor progression and metastasis.
ET(A) antagonism may curb ovarian carcinoma protease activity in vitro; leaves open translation to clinical progression or metastasis.
Endothelin-1 (ET-1) is a potent mitogenic and angiogenic factor for ovarian carcinoma cell lines, which acts selectively through the ET(A) receptor (ET(A)R). A previous study demonstrated that ET-1 is present at high concentrations in ovarian cancer ascites, indicating a direct role in the progression and metastasis of ovarian carcinoma. In this study, we investigated whether ET-1 could induce production and activation of tumour-associated proteinases in ovarian carcinoma cells. As demonstrated by ELISA, we found that the secretion of matrix metalloproteinase (MMP)-2 and MMP-9, urokinase-type plasminogen activator and plasminogen activator inhibitor type-1 and -2 was upregulated by ET-1 in a dose-dependent manner in the HEY cell line. In addition, the MMPs in ET-1-treated cells are consistently active, as shown by MMP gelatinase activity assay. Finally, we demonstrated that BQ-123, an antagonist of ET(A)R, inhibited the ET-1-induced tumour protease secretion and activity, suggesting that ET-1/ET(A)R may play an important role in the progression and metastasis of ovarian carcinoma, activating multiple proteinase cascades.
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Rosanò et al. (2002) studied Ovarian carcinoma. Endothelin-1 (ET-1) was evaluated on Secretion and activation of tumour-associated proteinases (MMP-2, MMP-9, uPA, PAI-1, PAI-2). Endothelin-1 upregulated the secretion and activity of tumour-associated proteinases in ovarian carcinoma cells, an effect inhibited by the ET(A) receptor antagonist BQ-123.
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