Momtaz Maryam, Rerat Vincent, Gharbi Sonia, Gérard Estelle, Pourcelle Vincent, Marchand-Brynaert Jacqueline
Unité de Chimie Organique et Médicinale, Université catholique de Louvain, 1 place Louis Pasteur, B-1348 Louvain-la-Neuve, Belgium.
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1084-90. doi: 10.1016/j.bmcl.2007.12.006. Epub 2007 Dec 8.
A graftable LDV (Leu-Asp-Val) peptidomimetic molecule (B-c) has been prepared from 3-(5-amino-2-hydroxy)phenyl-propionic acid, as alpha(4)beta(1) (VLA-4) integrin ligand. For that purpose, the mechanism of 3-(4-azidophenyl)propionic acid rearrangement has been revisited. Activation of Durapore DVPP-hydrophilic membrane, by surface wet chemistry using triazine trifluoride, followed by covalent coupling of B-c produced a modified filter (0.8% of derivatisation from XPS analysis) with improved capacity of leukocyte retention.
一种可移植的LDV（亮氨酸-天冬氨酸-缬氨酸）拟肽分子（B-c）已由3-(5-氨基-2-羟基)苯基丙酸制备而成，作为α(4)β(1)（VLA-4）整合素配体。为此，对3-(4-叠氮苯基)丙酸重排机制进行了重新研究。使用三嗪三氟化物通过表面湿化学方法对Durapore DVPP亲水膜进行活化，随后将B-c共价偶联，得到了一种改性滤膜（XPS分析显示衍生化率为0.8%），其白细胞保留能力得到了提高。
