氨基酸与肽。XXXII：纤连蛋白相关肽的双功能聚乙二醇杂化物。

Amino acids and peptides. XXXII: A bifunctional poly(ethylene glycol) hybrid of fibronectin-related peptides.

作者信息

Maeda M, Izuno Y, Kawasaki K, Kaneda Y, Mu Y, Tsutsumi Y, Lem K W, Mayumi T

机构信息

Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Japan.

出版信息

Biochem Biophys Res Commun. 1997 Dec 18;241(2):595-8. doi: 10.1006/bbrc.1997.7855.

DOI:10.1006/bbrc.1997.7855

PMID:9425317

Abstract

An amino acid type poly(ethylene glycol) (aaPPEG) was prepared and its application to a drug carrier was examined. The peptides, Arg-Gly-Asp (RGD) and Glu-Ile-Leu-Asp-Val (EILDV) which were reported as active fragments of Fibronectin (a cell adhesion protein), were conjugated with aaPEG (molecular weight, 10,000). The hybrid, RGD-aaPEG-EILDV, was prepared by a combination of the solid-phase method and the solution method. Antiadhesive activity of the peptides was not lost by its hybrid formation with the large aaPEG molecule. A mixture of RGD (0.43 mmol) and EILDV (0.43 mmol) did not demonstrate an antiadhesive effect, but the hybrid containing 0.43 mmol of each peptide did exhibit this effect.

摘要

制备了一种氨基酸型聚乙二醇（aaPPEG），并研究了其在药物载体中的应用。据报道，作为纤连蛋白（一种细胞粘附蛋白）活性片段的肽，精氨酸-甘氨酸-天冬氨酸（RGD）和谷氨酸-异亮氨酸-亮氨酸-天冬氨酸-缬氨酸（EILDV），与aaPEG（分子量10,000）偶联。通过固相法和溶液法相结合制备了杂合物RGD-aaPEG-EILDV。肽与大的aaPEG分子形成杂合物后，其抗粘附活性并未丧失。RGD（0.43 mmol）和EILDV（0.43 mmol）的混合物未表现出抗粘附作用，但每种肽各含0.43 mmol的杂合物确实表现出这种作用。