Preparation and Biological Activities of a Bivalent Poly(Ethylene Glycol) Hybrid Containing an Active Site and Its Synergistic Site of Fibronectin.
2002; Pharmaceutical Society of Japan; Volume: 50; Issue: 9 Linguagem: Inglês
10.1248/cpb.50.1229
ISSN1347-5223
AutoresYuichi Susuki, Keiko Hojo, Ikuko Okazaki, Haruhiko Kamata, Masahiko Sasaki, Mitsuko Maeda, Motoyoshi Nomizu, Yoko Yamamoto, Shinsaku Nakagawa, Tadanori Mayumi, Koichi Kawasaki,
Tópico(s)Monoclonal and Polyclonal Antibodies Research
ResumoA 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.
Referência(s)