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

被引：22

作者：

Susuki, Y

Hojo, K

Okazaki, I

Kamata, H

Sasaki, M

Maeda, M

Nomizu, M

Yamamoto, Y

Nakagawa, S

Mayumi, T

Kawasaki, K

机构：

[1] Kobe Gakuin Univ, Fac Pharmaceut Sci, Nishi Ku, Kobe, Hyogo 6512180, Japan

[2] Kobe Gakuin Univ, High Technol Res Ctr, Nishi Ku, Kobe, Hyogo 6512180, Japan

[3] Hokkaido Univ, Grad Sch Environm Earth Sci, Sapporo, Hokkaido 0600810, Japan

[4] Osaka Univ, Grad Sch Pharmaceut Sci, Suita, Osaka 5650871, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2002年 / 50卷 / 09期

关键词：

poly(ethylene glycol); fibronectin; hybrid; spreading activity; anti-metastatic activity;

D O I：

10.1248/cpb.50.1229

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1229 / 1232

页数：4

共 24 条

[1]

AOTA S, 1994, J BIOL CHEM, V269, P24756

[2] 9-FLUORENYLMETHOXYCARBONYL FUNCTION, A NEW BASE-SENSITIVE AMINO-PROTECTING GROUP [J].