A serum-stable branched dimeric anti-VEGF peptide blocks tumor growth via anti-angiogenic activity
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- Title
- A serum-stable branched dimeric anti-VEGF peptide blocks tumor growth via anti-angiogenic activity
- Authors
- Kim, JW; Kim, TD; Hong, BS; Kim, OY; Yoon, WH; Chae, CB; Gho, YS
- Date Issued
- 2010-07-31
- Publisher
- KOREAN SOC MED BIOCHEMISTRY MOLECULAR BIOLOGY
- Abstract
- Angiogenesis is critical and indispensable for tumor progression. Since VEGF is known to play a central role in angiogenesis, the disruption of VEGF-VEGF receptor system is a promising target for anti-cancer therapy. Previously, we reported that a hexapeptide (RRKRRR, RK6) blocked the growth and metastasis of tumor by inhibiting VEGF binding to its receptors. In addition, dRK6, the D-form derivative of RK6, retained its biological activity with improved serum stability. In the present study, we developed a serum-stable branched dimeric peptide (MAP2-dRK6) with enhanced anti-VEGF and anti-tumor activity. MAP2-dRK6 is more effective than dRK6 in many respects: inhibition of VEGF binding to its receptors, VEGF- and tumor conditioned medium-induced proliferation and ERK signaling of endothelial cells, and VEGF-induced migration and tube formation of endothelial cells. Moreover, MAP2-dRK6 blocks in vivo growth of VEGF-secreting colorectal cancer cells by the suppression of angiogenesis and the subsequent induction of tumor cell apoptosis. Our observations suggest that MAP2-dRK6 can be a prospective therapeutic molecule or lead compound for the development of drugs for various VEGF-related angiogenic diseases.
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/10201
- DOI
- 10.3858/EMM.2010.42.7.052
- ISSN
- 1226-3613
- Article Type
- Article
- Citation
- EXPERIMENTAL AND MOLECULAR MEDICINE, vol. 42, no. 7, page. 514 - 523, 2010-07-31
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