Validation of 57 Tag-lite ligand binding assay starter packs. Correlation of agonist and antagonist Ki obtained with Tag-lite and radioactive ligand binding assays
Roux T, Tardieu JL, Leyris JP, Marie J, Fink M, Douzon S, Douayry N, Costy N, LeBlay M
Cisbio Bioassays, Codolet, France. Institut de Genomique Fonctionnelle, Montpellier, France.
SBS 17th Annual Conference. April 2011, Orlando, USA
Ligand binding assays which investigate the first step of the drug receptor interaction remain a method of choice when investigating drug effects. Despite the constraints associated with the use of a radioactive ligand (including delivery, disposal of radioactive material, half-life and radiolysis of compounds inducing short shelf-life of the ligand) radioactive methods remain the gold standard in receptor ligand binding assays. Nevertheless, homogeneous and non-radioactive alternatives are being investigated to provide HTS assays. An additional incentive is that some ligands have induced a high non-specific binding (NSB) making radioligand assays time-consuming to develop (e.g. chemokine assays). Tag-lite is a new homogeneous and non-radioactive cell-based platform developed by Cisbio Bioassays to address ligand receptor interaction. All these assays are available under a ready-to-use starter pack format containing the fluorescent ligand and the pre-labeled frozen cells. To date, 57 fully validated GPCR packs are available.