title: Identification of a novel peptide ligand of human vascular endothelia growth factor receptor 3 for targeted tumour diagnosis and therapy.
abstract: Human vascular endothelia growth factor receptor 3 (VEGFR-3) is up-regulated in a variety of human cancers. It is a potentially rational target for drug delivery. To identify novel ligands with specific binding capabilities to VEGFR-3, we screened a phage display peptide library and found a consensus motif of the peptides which is displayed by the positive phages CSDxxHxWC (x is any amino acid). The phage displaying peptide CSDSWHYWC (designated as P1) exhibited the highest affinity to VEGFR-3 in phage ELISA and the chemically synthesized P1 could bind to VEGFR-3 specifically in a dose-dependent manner. In addition, the flow cytometry assay and immunofluorescence showed that the FITC labelled P1 could bind to VEGFR-3 positive carcinoma cells with specificity. Our study suggests that P1 may be a homing peptide for treatment of tumours.
authors.affiliation: Biotechnology Center of The Fourth Military Medical University, and State Key Laboratory of Cancer Biology, 17 Chang'le West Road, 710032 Xi'an, People's Republic of China.
authors.forename: Xin
authors.initials: X
authors.lastname: Qin
authors.forename: Yi
authors.initials: Y
authors.lastname: Wan
authors.forename: Meng
authors.initials: M
authors.lastname: Li
authors.forename: Xiaochang
authors.initials: X
authors.lastname: Xue
authors.forename: Shouzhen
authors.initials: S
authors.lastname: Wu
authors.forename: Cun
authors.initials: C
authors.lastname: Zhang
authors.forename: Yanjie
authors.initials: Y
authors.lastname: You
authors.forename: Weihua
authors.initials: W
authors.lastname: Wang
authors.forename: Changli
authors.initials: C
authors.lastname: Jiang
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.forename: Wenhua
authors.initials: W
authors.lastname: Zhu
authors.forename: Yonggang
authors.initials: Y
authors.lastname: Ran
authors.forename: Zhen
authors.initials: Z
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Han
authors.forename: Yingqi
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000595:Amino Acid Sequence; D001665:Binding Sites; D045744:Cell Line, Tumor; D030562:Databases, Protein; D042783:Endothelial Cells / Q000378:metabolism; D005434:Flow Cytometry; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry / Q000378:metabolism; D005455:Fluorescent Antibody Technique; D006801:Humans; D008024:Ligands; D008969:Molecular Sequence Data; D009369:Neoplasms / Q000175:diagnosis / Q000188:drug therapy* / Q000378:metabolism; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D019151:Peptide Library; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D040321:Vascular Endothelial Growth Factor Receptor-3 / Q000378:metabolism*
chemical_list: D008024:Ligands; D009842:Oligopeptides; D019151:Peptide Library; D010455:Peptides; C524412:cysteinyl-seryl-aspartyl-seryl-tryptophyl-histidyl-tyrosyl-tryptophyl-cysteine; D040321:Vascular Endothelial Growth Factor Receptor-3; D016650:Fluorescein-5-isothiocyanate