Novel peptides suppress VEGFR-3 activity and antagonize VEGFR-3-mediated oncogenic effects

Yi Wen Chang, Chih Ming Su, Yen Hao Su, Yuan Soon Ho, Hui Huang Lai, Hsin An Chen, Min Liang Kuo, Wen Chun Hung, Ya Wen Chen, Chih Hsiung Wu, Pai Sheng Chen, Jen Liang Su

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Vascular endothelial growth factor receptor 3 (VEGFR-3) supports tumor lymphangiogenesis. It was originally identified as a lymphangiogenic factor expressed in lymphatic endothelial cells. VEGFR-3 was detected in advanced human malignancies and correlated with poor prognosis. Our previous studies show that activation of the VEGF-C/VEGFR-3 axis promotes cancer metastasis and is associated with clinical progression in patients with lung cancer, indicating that VEGFR-3 is a potential target for cancer therapy. In this study, we developed eight peptides targeting VEGFR-3. Two peptides strongly inhibited the kinase activity of VEGFR-3 and suppressed VEGF-C-mediated invasion of cancer cells. Moreover, these peptides abolished VEGF-C-induced drug resistance and tumor initiating cell formation. This study demonstrates the therapeutic potential of VEGFR-3-targeting peptides.

Original languageEnglish
Pages (from-to)3823-3835
Number of pages13
JournalOncotarget
Volume5
Issue number11
DOIs
Publication statusPublished - 2014

Fingerprint

Vascular Endothelial Growth Factor Receptor-3
Peptides
Vascular Endothelial Growth Factor C
Neoplasms
Lymphangiogenesis
Neoplastic Stem Cells
Drug Resistance
Lung Neoplasms
Phosphotransferases
Endothelial Cells
Neoplasm Metastasis
Therapeutics

All Science Journal Classification (ASJC) codes

  • Oncology

Cite this

Chang, Y. W., Su, C. M., Su, Y. H., Ho, Y. S., Lai, H. H., Chen, H. A., ... Su, J. L. (2014). Novel peptides suppress VEGFR-3 activity and antagonize VEGFR-3-mediated oncogenic effects. Oncotarget, 5(11), 3823-3835. https://doi.org/10.18632/oncotarget.1709
Chang, Yi Wen ; Su, Chih Ming ; Su, Yen Hao ; Ho, Yuan Soon ; Lai, Hui Huang ; Chen, Hsin An ; Kuo, Min Liang ; Hung, Wen Chun ; Chen, Ya Wen ; Wu, Chih Hsiung ; Chen, Pai Sheng ; Su, Jen Liang. / Novel peptides suppress VEGFR-3 activity and antagonize VEGFR-3-mediated oncogenic effects. In: Oncotarget. 2014 ; Vol. 5, No. 11. pp. 3823-3835.
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Chang, YW, Su, CM, Su, YH, Ho, YS, Lai, HH, Chen, HA, Kuo, ML, Hung, WC, Chen, YW, Wu, CH, Chen, PS & Su, JL 2014, 'Novel peptides suppress VEGFR-3 activity and antagonize VEGFR-3-mediated oncogenic effects', Oncotarget, vol. 5, no. 11, pp. 3823-3835. https://doi.org/10.18632/oncotarget.1709

Novel peptides suppress VEGFR-3 activity and antagonize VEGFR-3-mediated oncogenic effects. / Chang, Yi Wen; Su, Chih Ming; Su, Yen Hao; Ho, Yuan Soon; Lai, Hui Huang; Chen, Hsin An; Kuo, Min Liang; Hung, Wen Chun; Chen, Ya Wen; Wu, Chih Hsiung; Chen, Pai Sheng; Su, Jen Liang.

In: Oncotarget, Vol. 5, No. 11, 2014, p. 3823-3835.

Research output: Contribution to journalArticle

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AU - Chang, Yi Wen

AU - Su, Chih Ming

AU - Su, Yen Hao

AU - Ho, Yuan Soon

AU - Lai, Hui Huang

AU - Chen, Hsin An

AU - Kuo, Min Liang

AU - Hung, Wen Chun

AU - Chen, Ya Wen

AU - Wu, Chih Hsiung

AU - Chen, Pai Sheng

AU - Su, Jen Liang

PY - 2014

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AB - Vascular endothelial growth factor receptor 3 (VEGFR-3) supports tumor lymphangiogenesis. It was originally identified as a lymphangiogenic factor expressed in lymphatic endothelial cells. VEGFR-3 was detected in advanced human malignancies and correlated with poor prognosis. Our previous studies show that activation of the VEGF-C/VEGFR-3 axis promotes cancer metastasis and is associated with clinical progression in patients with lung cancer, indicating that VEGFR-3 is a potential target for cancer therapy. In this study, we developed eight peptides targeting VEGFR-3. Two peptides strongly inhibited the kinase activity of VEGFR-3 and suppressed VEGF-C-mediated invasion of cancer cells. Moreover, these peptides abolished VEGF-C-induced drug resistance and tumor initiating cell formation. This study demonstrates the therapeutic potential of VEGFR-3-targeting peptides.

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