Use of a fluorescent polarization based high throughput assay to identify new Calmodulin ligands

被引：21

作者：

Dagher, Rania

Pigault, Claire

Bonnet, Dominique

Boeglin, Damien

Pourbaix, Christelle

Kilhoffer, Marie-Claude

Villa, Pascal

Wermuth, Camille G.

Hibert, Marcel

Haiech, Jacques

机构：

[1] Fac Pharm, IFR85, Plateforme Chim Biol Integrat Strasbourg, F-67401 Illkirch Graffenstaden, France

[2] Prestwick Chem Inc, F-67400 Illkirch Graffenstaden, France

来源：

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH | 2006年 / 1763卷 / 11期

关键词：

fluorescence polarization/anisotropy; FP-high-throughput screening; synCaM; fluorescent peptides based library;

D O I：

10.1016/j.bbamcr.2006.09.027

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：

In order to develop a fluorescence polarization (FP) assay for calcium binding proteins, a fluorescent peptides based library of 1328 compounds has been synthesized. The use of this library has been validated by setting up a FP-high-throughput screening (FP-HTS) assay for calmodulin using the synthetic gene product (synCaM). With this assay, a set of 880 FDA approved compounds was screened. Besides the promazine class, we discovered two new classes of compounds that interact with calmodulin in a calcium dependent manner. One class has compounds with anti-histaminic/spasmolytic activities, and the other one are detergents with antibacterial activities. (c) 2006 Elsevier B.V. All rights reserved.

引用

页码：1250 / 1255

页数：6

共 17 条

[11]

RENAULT F, UNPUB INTRACELLULAR

[12] SOLID-PHASE SYNTHESIS OF PROTECTED PEPTIDE-FRAGMENTS USING A TRIALKOXY-DIPHENYL-METHYLESTER RESIN [J].