Abstract
Matriptase is an epithelia-specific membrane-anchored serine protease that has received considerable attention in recent years because of its consistent dysregulation in human epithelial tumours, including breast cancer. Mice with reduced levels of matriptase display a significant delay in oncogene-induced mammary tumour formation and blunted tumour growth. The abated tumour growth is associated with a decrease in cancer cell proliferation. Here we demonstrate by genetic deletion and silencing that the proliferation impairment in matriptase-deficient breast cancer cells is caused by their inability to initiate activation of the c-Met signalling pathway in response to fibroblast-secreted pro-HGF. Similarly, inhibition of matriptase catalytic activity using a selective small-molecule inhibitor abrogates the activation of c-Met, Gab1 and AKT, in response to pro-HGF, which functionally leads to attenuated proliferation in breast carcinoma cells. We conclude that matriptase is critically involved in breast cancer progression and represents a potential therapeutic target in breast cancer.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Adaptor Proteins, Signal Transducing
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Animals
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Blotting, Western
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Breast Neoplasms / genetics*
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Breast Neoplasms / metabolism
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Carcinoma / genetics*
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Carcinoma / metabolism
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Cell Culture Techniques
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Cell Line, Tumor
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Cell Proliferation / genetics*
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Female
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Hepatocyte Growth Factor / metabolism*
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Humans
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Immunohistochemistry
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Mammary Neoplasms, Animal / genetics
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Mammary Neoplasms, Animal / metabolism
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Mammary Neoplasms, Experimental / genetics*
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Mammary Neoplasms, Experimental / metabolism
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Membrane Proteins / genetics*
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Mice
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Mice, Knockout
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Mice, Transgenic
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Phosphoproteins
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Protein Precursors / metabolism*
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Proto-Oncogene Proteins c-akt
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Proto-Oncogene Proteins c-met
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Serine Endopeptidases / genetics*
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Signal Transduction
Substances
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Adaptor Proteins, Signal Transducing
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GAB1 protein, human
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Gab1 protein, mouse
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Membrane Proteins
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Phosphoproteins
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Protein Precursors
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pro-hepatocyte growth factor
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Hepatocyte Growth Factor
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Proto-Oncogene Proteins c-met
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Proto-Oncogene Proteins c-akt
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Serine Endopeptidases
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ST14 protein, human
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St14 protein, mouse