High-Affinity Functional Fluorescent Ligands for Human β-Adrenoceptors.

ABSTRACT: Visualization of the G-protein coupled receptor (GPCR) is of great importance for studying its function in a native cell. We have synthesized a series of red-emitting fluorescent probes targeting β-adrenergic receptor (βAR) that are compatible with confocal and Stimulated Emission Depletion (STED) microscopy as well as with Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) binding assay in living cells. The probe based on the agonist BI-167107 and fluorescent dye KK114 demonstrates nanomolar binding affinity and up to nine-fold β₂AR selectivity over β₁AR. Carazolol-derived probes are fluorogenic and allow no-wash imaging experiments. STED microscopy of β₂ARs stained at the native expression level on pancreatic CAPAN cells provides two-fold impr

SUBMITTER: Mitronova GY 

PROVIDER: S-EPMC5614969 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature