title: Use of a fluorescent polarization based high throughput assay to identify new calmodulin ligands.
abstract: 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.
authors.affiliation: UMR 7175- LC1, Institut Gilbert Laustriat, Département de Pharmacochimie de la Communication Cellulaire, France.
authors.forename: Rania
authors.initials: R
authors.lastname: Dagher
authors.forename: Claire
authors.initials: C
authors.lastname: Pigault
authors.forename: Dominique
authors.initials: D
authors.lastname: Bonnet
authors.forename: Damien
authors.initials: D
authors.lastname: Boeglin
authors.forename: Christelle
authors.initials: C
authors.lastname: Pourbaix
authors.forename: Marie-Claude
authors.initials: MC
authors.lastname: Kilhoffer
authors.forename: Pascal
authors.initials: P
authors.lastname: Villa
authors.forename: Camille G
authors.initials: CG
authors.lastname: Wermuth
authors.forename: Marcel
authors.initials: M
authors.lastname: Hibert
authors.forename: Jacques
authors.initials: J
authors.lastname: Haiech
mesh_terms: D002135:Calcium-Binding Proteins / Q000737:chemistry* / Q000235:genetics; D002147:Calmodulin / Q000737:chemistry* / Q000235:genetics; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D005454:Fluorescence Polarization / Q000379:methods*; D008024:Ligands; D019151:Peptide Library; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D002135:Calcium-Binding Proteins; D002147:Calmodulin; D008024:Ligands; D019151:Peptide Library; D010455:Peptides