title: 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.affiliation: Graduate Institute of Clinical Medicine, Taipei Medical University, Taipei 11031, Taiwan.
authors.forename: Chia-Che
authors.initials: CC
authors.lastname: Wu
authors.forename: Erh-Hsuan
authors.initials: EH
authors.lastname: Lin
authors.forename: Yu-Ching
authors.initials: YC
authors.lastname: Lee
authors.forename: Cheng-Jeng
authors.initials: CJ
authors.lastname: Tai
authors.forename: Tsu-Hsiang
authors.initials: TH
authors.lastname: Kuo
authors.forename: Hsin-Ell
authors.initials: HE
authors.lastname: Wang
authors.forename: Tsai-Yueh
authors.initials: TY
authors.lastname: Luo
authors.forename: Ying-Kai
authors.initials: YK
authors.lastname: Fu
authors.forename: Haw-Jan
authors.initials: HJ
authors.lastname: Chen
authors.forename: Ming-Ding
authors.initials: MD
authors.lastname: Sun
authors.forename: Chih-Hsiung
authors.initials: CH
authors.lastname: Wu
authors.forename: Cheng-Wen
authors.initials: CW
authors.lastname: Wu
authors.forename: Sy-Jye
authors.initials: SJ
authors.lastname: Leu
authors.forename: Win-Ping
authors.initials: WP
authors.lastname: Deng
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D045744:Cell Line, Tumor; D003952:Diagnostic Imaging / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D005353:Fibronectins / Q000494:pharmacology; D005354:Fibrosarcoma / Q000175:diagnosis* / Q000378:metabolism / Q000628:therapy*; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D019151:Peptide Library; D010455:Peptides / Q000032:analysis* / Q000737:chemistry; D011485:Protein Binding / Q000187:drug effects; D014018:Tissue Distribution / Q000187:drug effects
chemical_list: D005353:Fibronectins; D019151:Peptide Library; D010455:Peptides