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

Date publication

novembre 2006

Auteurs

Membres identifiés du Cancéropôle Est :
Pr HAIECH Jacques , Pr HIBERT Marcel

Tous les auteurs :
Dagher R, Pigault C, Bonnet D, Boeglin D, Pourbaix C, Kilhoffer MC, Villa P, Wermuth CG, Hibert M, Haiech J

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/17081635

Résumé

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.

Référence

Biochim Biophys Acta. 2006 Nov;1763(11):1250-5