Identification of novel anthrax lethal factor inhibitors generated by combinatorial Pictet-Spengler reaction followed by screening in situ

被引：36

作者：

Numa, MMD

Lee, LV

Hsu, CC

Bower, KE

Wong, CH

机构：

[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA

[3] Scripps Res Inst, Div Oncovirol, Dept Mol & Expt Med, La Jolla, CA 92037 USA

来源：

CHEMBIOCHEM | 2005年 / 6卷 / 06期

关键词：

anthrax; carbohydrates; combinatorial chemistry; inhibitors; Pictet-Spengler;

D O I：

10.1002/cbic.200500009

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：

Potent library. Anthrax lethal factor (LF) is a zinc-dependent metalloprotease involved in the rapid development of the deadly infection caused by Bacillus anthracis. Blocking its action is a plausible method to mitigate the deleterious effects of late stage infection. We report the inhibition of LF by tetrahydro-isoquinoline polyphenolic compounds, such as 5a, which were identified by screening a combinatorial library that was generated by Pictet-Spengler reaction. We also report the identification of commercially available polyphenolic inhibitors against LF. © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：1002 / 1006

页数：5

共 32 条

[1] Anthrax toxin triggers endocytosis of its receptor via a lipid raft-mediated clathrin-dependent process [J].