Development of a high-throughput calcium flux assay for identification of all ligand types including positive, negative, and silent allosteric modulators for G protein-coupled receptors.
Assay Drug Dev Technol
; 10(5): 457-67, 2012 Oct.
Article
em En
| MEDLINE
| ID: mdl-22746835
ABSTRACT
In recent years, the increased use of cell-based functional assays for G protein-coupled receptors in high-throughput screening has enabled the design of robust assays to identify allosteric modulators (AMs) in addition to the more traditional orthosteric agonists and antagonists. In this article, the authors describe a screening format able to identify all ligand types using a triple-add assay that measures changes in cytosolic calcium concentration with three separate additions and reads in the same assay plate. This triple-add assay captures more small molecule ligand types than previously described assay formats without a significant increase in screening cost. Finally, the customizability of the triple-add assay to suit the needs of various AM screening programs is demonstrated.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sinalização do Cálcio
/
Receptores Acoplados a Proteínas G
/
Ensaios de Triagem em Larga Escala
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article