Searching for the most effective screening system to identify cell-active inhibitors of β-secretase

被引：11

作者：

Middendorp, O ^{[1
]}

Lüthi, U ^{[1
]}

Hausch, F ^{[1
]}

Barberis, A ^{[1
]}

机构：

[1] ESBATech AG, CH-8952 Zurich, Switzerland

来源：

BIOLOGICAL CHEMISTRY | 2004年 / 385卷 / 06期

关键词：

A beta; Alzheimer's disease; BACE1; beta-secretase; beta-secretase inhibitor; screening system;

D O I：

10.1515/BC.2004.056

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The P-secretase BACE1 is an attractive drug target for reducing the level of the Alzheimer's disease-promoting Abeta peptide in the brain. Whereas potent peptidomimetic in vitro inhibitors of BACE1 have been designed, screening approaches to identify cell-permeable small molecule inhibitors have had limited success so far. In the present minireview we summarize existing screening methods, discuss their scope of application in the drug discovery process and compare them to a novel cell-based screening system to identify BACE1 inhibitors by a positive yeast growth selection.

引用

页码：481 / 485

页数：5

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