Synthesis and enzymatic evaluation of a P1 arginine aminocoumarin substrate library for trypsin-like serine proteases

被引：38

作者：

Edwards, PD

Mauger, RC

Cottrell, KM

Morris, FX

Pine, KK

Sylvester, MA

Scott, CW

Furlong, ST

机构：

[1] AstraZeneca Pharmaceut, Dept Chem, Wilmington, DE 19850 USA

[2] AstraZeneca Pharmaceut, Dept Neurosci, Wilmington, DE 19850 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(00)00460-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A method for the solid-phase synthesis of P-1 arginine containing peptides via attachment of the arginine side-chain guanidine group is described. This procedure is applied to the preparation of a tetrapeptide, P-1 arginine aminocoumarin PS-SCL. This library was validated by using it to determine the P-4-P-2 specificity for thrombin and comparing the results to the known thrombin subsite specificity. This is the first reported example of a PS-SCL library containing a P-1 arginine. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2291 / 2294

页数：4

共 10 条

[1] Synthesis of positional-scanning libraries of fluorogenic peptide substrates to define the extended substrate specificity of plasmin and thrombin [J].