A novel small peptide as a targeting ligand for receptor tyrosine kinase Tie2 |
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Authors: | Wu Xianghua Zhao Ruijiao Li Zonghai Yao Ming Wang Huamao Han Junsong Qu Shumin Chen Xianlian Qian Lianfang Sun Ye Xu Yuhong Gu Jianren |
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Affiliation: | National Laboratory for Oncogenes and Related Genes, Shanghai Cancer Institute, Shanghai Jiao-Tong University Medical School, Shanghai 200032, PR China. |
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Abstract: | Tie2 is an endothelium-specific receptor tyrosine kinase known to play an important role in tumor angiogenesis. We sought to identify a small peptide ligand against Tie2 for developing a delivery targeting agent. We used hydrophobic analysis and comparative sequence/structure analysis to select a minimal peptide based on angiopoietin-2 amino acid sequence. The resulting peptide named GA3(WTIIQRREDGSVDFQRTWKEYK) was synthesized and labeled with iodine-125 at the C-terminal tyrosine residue to characterize its binding capability. In in vitro binding assays, GA3 can not only specifically bind to SMMC7721-Tie2 but also compete with angiopoietin-2 in binding. Via mouse tail vein injection, 125I-labeled GA3 was found to favorably accumulate in SPC-A1 xenograft tumor tissues which positively express Tie2. These results demonstrated that GA3 may be useful as a drug or gene delivery ligand for targeted chemotherapy, radiotherapy, and gene therapy. |
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Keywords: | Tie2 Angiogenesis Peptide ligand Tumor targeting Angiopoietin-2 |
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