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

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.

Improved preparation of an amino acid type poly(ethylene glycol) derivative.

An amino acid type poly(ethylene glycol) is a useful tool for preparation of a bi- or multivalent poly(ethylene glycol) hybrid of bioactive peptides, but synthesis is problematic. The amino acid type poly(ethylene glycol) was prepared from poly(oxyethylene)diglycolic acid followed by introduction of a fluorenylmethyloxycarbonyl group. The resulting product could be purified easily by LH-20 column chromatography and HPLC.