title: Preparation and biological activities of a bivalent poly(ethylene glycol) hybrid containing an active site and its synergistic site of fibronectin.
abstract: A bivalent poly(ethylene glycol) or PEG hybrid of fibronectin-related peptides was prepared. An active site peptide (RGD) and its synergistic site peptide (PHSRN) of fibronectin were conjugated with an amino acid-type PEG (aaPEG) to form PHSRN-aaPEG-RGD. A moderate spatial array between RGD and PHSRN in fibronectin may be required for synergic activity. The bivalent hybrid exhibited potent cell spreading activity and exhibited potent anti-metastatic activity in a model of experimental metastasis with B16-BL6 cells in mice. PEG may serve as a spacer for maintaining the desired spatial array.
authors.affiliation: Faculty of Pharmaceutical Sciences and High Technology Research Center, Kobe Gakuin University, Japan.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Susuki
authors.forename: Keiko
authors.initials: K
authors.lastname: Hojo
authors.forename: Ikuko
authors.initials: I
authors.lastname: Okazaki
authors.forename: Haruhiko
authors.initials: H
authors.lastname: Kamata
authors.forename: Masahiko
authors.initials: M
authors.lastname: Sasaki
authors.forename: Mitsuko
authors.initials: M
authors.lastname: Maeda
authors.forename: Motoyoshi
authors.initials: M
authors.lastname: Nomizu
authors.forename: Yoko
authors.initials: Y
authors.lastname: Yamamoto
authors.forename: Shinsaku
authors.initials: S
authors.lastname: Nakagawa
authors.forename: Tadanori
authors.initials: T
authors.lastname: Mayumi
authors.forename: Koichi
authors.initials: K
authors.lastname: Kawasaki
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D002470:Cell Survival; D002851:Chromatography, High Pressure Liquid; D006224:Cricetinae; D005353:Fibronectins / Q000737:chemistry*; D007202:Indicators and Reagents; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D008810:Mice, Inbred C57BL; D009362:Neoplasm Metastasis / Q000473:pathology / Q000517:prevention & control; D009368:Neoplasm Transplantation; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000596:Amino Acids; D000970:Antineoplastic Agents; D005353:Fibronectins; D007202:Indicators and Reagents; D011092:Polyethylene Glycols