Preparation and biological activities of a bivalent poly(ethylene glycol) hybrid containing an active site and its synergistic site of fibronectin.

نویسندگان

  • Yuichi Susuki
  • Keiko Hojo
  • Ikuko Okazaki
  • Haruhiko Kamata
  • Masahiko Sasaki
  • Mitsuko Maeda
  • Motoyoshi Nomizu
  • Yoko Yamamoto
  • Shinsaku Nakagawa
  • Tadanori Mayumi
  • Koichi Kawasaki
چکیده

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.

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عنوان ژورنال:
  • Chemical & pharmaceutical bulletin

دوره 50 9  شماره 

صفحات  -

تاریخ انتشار 2002