E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion
<p>Abstract</p> <p>Background</p> <p>E7080 is an orally active multi-targeted kinase inhibitor whose targets include vascular endothelial growth factor receptors (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptors (PDGFR). It h...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
BMC
2011-07-01
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| Series: | BMC Cancer |
| Online Access: | http://www.biomedcentral.com/1471-2407/11/309 |
| _version_ | 1818390297642532864 |
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| author | Macleod Kenneth Patel Hitesh Mason Susan Glen Hilary Brunton Valerie G |
| author_facet | Macleod Kenneth Patel Hitesh Mason Susan Glen Hilary Brunton Valerie G |
| author_sort | Macleod Kenneth |
| collection | DOAJ |
| description | <p>Abstract</p> <p>Background</p> <p>E7080 is an orally active multi-targeted kinase inhibitor whose targets include vascular endothelial growth factor receptors (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptors (PDGFR). It has been shown to inhibit tumor angiogenesis by targeting endothelial cells. A number of the targets of E7080 are also expressed on tumor cells and here we have looked at the direct effects of E7080 on tumor cell behavior.</p> <p>Methods</p> <p>Using a panel of human tumor cell lines we determined the effect of E7080 on cell proliferation, migration and invasion. Inhibition of FGFR and PDGFR signaling in the cells was measured.</p> <p>Results</p> <p>E7080 had little effect on tumor cell proliferation. However, it blocked migration and invasion at concentrations that inhibited FGFR and PDGFR signaling. Knock-down of PDGFR-β in U2OS osteosarcoma cells also inhibited cell migration which, could not be further inhibited in the presence of E7080. Furthermore, E7080 could not inhibit the migration of a PDGFR negative cell line.</p> <p>Conclusion</p> <p>E7080 does not significantly affect tumor cell proliferation but can inhibit their migration and invasion at concentrations that both inhibit its known targets and are achievable clinically.</p> |
| first_indexed | 2024-12-14T04:55:24Z |
| format | Article |
| id | doaj.art-d41d8dee428742ee8b83e36eb32c07f5 |
| institution | Directory Open Access Journal |
| issn | 1471-2407 |
| language | English |
| last_indexed | 2024-12-14T04:55:24Z |
| publishDate | 2011-07-01 |
| publisher | BMC |
| record_format | Article |
| series | BMC Cancer |
| spelling | doaj.art-d41d8dee428742ee8b83e36eb32c07f52022-12-21T23:16:23ZengBMCBMC Cancer1471-24072011-07-0111130910.1186/1471-2407-11-309E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasionMacleod KennethPatel HiteshMason SusanGlen HilaryBrunton Valerie G<p>Abstract</p> <p>Background</p> <p>E7080 is an orally active multi-targeted kinase inhibitor whose targets include vascular endothelial growth factor receptors (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptors (PDGFR). It has been shown to inhibit tumor angiogenesis by targeting endothelial cells. A number of the targets of E7080 are also expressed on tumor cells and here we have looked at the direct effects of E7080 on tumor cell behavior.</p> <p>Methods</p> <p>Using a panel of human tumor cell lines we determined the effect of E7080 on cell proliferation, migration and invasion. Inhibition of FGFR and PDGFR signaling in the cells was measured.</p> <p>Results</p> <p>E7080 had little effect on tumor cell proliferation. However, it blocked migration and invasion at concentrations that inhibited FGFR and PDGFR signaling. Knock-down of PDGFR-β in U2OS osteosarcoma cells also inhibited cell migration which, could not be further inhibited in the presence of E7080. Furthermore, E7080 could not inhibit the migration of a PDGFR negative cell line.</p> <p>Conclusion</p> <p>E7080 does not significantly affect tumor cell proliferation but can inhibit their migration and invasion at concentrations that both inhibit its known targets and are achievable clinically.</p>http://www.biomedcentral.com/1471-2407/11/309 |
| spellingShingle | Macleod Kenneth Patel Hitesh Mason Susan Glen Hilary Brunton Valerie G E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion BMC Cancer |
| title | E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion |
| title_full | E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion |
| title_fullStr | E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion |
| title_full_unstemmed | E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion |
| title_short | E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion |
| title_sort | e7080 a multi targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion |
| url | http://www.biomedcentral.com/1471-2407/11/309 |
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