Identification of a new peptide for fibrosarcoma tumor targeting and imaging in vivo.

Abstract

A 12-mer amino acid peptide SATTHYRLQAAN, denominated TK4, was isolated from a phage-display library with fibrosarcoma tumor-binding activity. In vivo biodistribution analysis of TK4-displaying phage showed a significant increased phage titer in implanted tumor up to 10-fold in comparison with normal tissues after systemic administration in mouse. Competition assay confirmed that the binding of TK4-phage to tumor cells depends on the TK4 peptide. Intravenous injection of (131)I-labeled synthetic TK4 peptide in mice showed a tumor retention of 3.3% and 2.7% ID/g at 1- and 4-hour postinjection, respectively. Tumor-to-muscle ratio was 1.1, 5.7, and 3.2 at 1-, 4-, and 24-hour, respectively, and tumors were imaged on a digital γ-camera at 4-hour postinjection. The present data suggest that TK4 holds promise as a lead structure for tumor targeting, and it could be further applied in the development of diagnostic or therapeutic agent.

• Authors: Chia-Che Wu, Erh-Hsuan Lin, Yu-Ching Lee, Cheng-Jeng Tai, Tsu-Hsiang Kuo, Hsin-Ell Wang, Tsai-Yueh Luo, Ying-Kai Fu, Haw-Jan Chen, Ming-Ding Sun, Chih-Hsiung Wu, Cheng-Wen Wu, Sy-Jye Leu, Win-Ping Deng
• Journal: Journal of biomedicine & biotechnology (J Biomed Biotechnol) Vol. 2010 Pg. 167045 ( 2010) ISSN: 1110-7251 [Electronic] United States
• PMID: 21151669 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Fibronectins
• Peptide Library
• Peptides

Topics

• Amino Acid Sequence
• Animals
• Cell Line, Tumor
• Diagnostic Imaging (methods)
• Drug Delivery Systems (methods)
• Female
• Fibronectins (pharmacology)
• Fibrosarcoma (diagnosis, metabolism, therapy)
• Humans
• Mice
• Molecular Sequence Data
• Peptide Library
• Peptides (analysis, chemistry)
• Protein Binding (drug effects)
• Tissue Distribution (drug effects)