Identification of a novel peptide ligand of human vascular endothelia growth factor receptor 3 for targeted tumour diagnosis and therapy.
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.
Qin
Xin
X
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.
Wan
Yi
Y
Li
Meng
M
Xue
Xiaochang
X
Wu
Shouzhen
S
Zhang
Cun
C
You
Yanjie
Y
Wang
Weihua
W
Jiang
Changli
C
Liu
Yan
Y
Zhu
Wenhua
W
Ran
Yonggang
Y
Zhang
Zhen
Z
Han
Wei
W
Zhang
Yingqi
Y
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*
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