Fluorescence based HTS-compatible ligand binding assays for dopamine D₃ receptors in baculovirus preparations and live cells.

ABSTRACT: Dopamine receptors are G-protein-coupled receptors that are connected to severe neurological disorders. The development of new ligands targeting these receptors enables gaining a deeper insight into the receptor functioning, including binding mechanisms, kinetics and oligomerization. Novel fluorescent probes allow the development of more efficient, cheaper, reliable and scalable high-throughput screening systems, which speeds up the drug development process. In this study, we used a novel Cy3B labelled commercially available fluorescent ligand CELT-419 for developing dopamine D3 receptor-ligand binding assays with fluorescence polarization and quantitative live cell epifluorescence microscopy. The fluorescence anisotropy assay using 384-well plates achieved Z' value of 0.71, which is suita

SUBMITTER: Tahk MJ 

PROVIDER: S-EPMC10062709 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature