A_2AR Binding Kinetics in the Ligand Depletion Regime.

ABSTRACT: Ligand binding plays a fundamental role in stimulating the downstream signaling of membrane receptors. Here, ligand-binding kinetics of the full-length human adenosine A_2A receptor (A_2AR) reconstituted in detergent micelles were measured using a fluorescently labeled ligand via fluorescence anisotropy. Importantly, to optimize the signal-to-noise ratio, these experiments were conducted in the ligand depletion regime. In the ligand depletion regime, the assumptions used to determine analytical solutions for one-site binding models for either one or two ligands in competition are no longer valid. We therefore implemented a numerical solution approach to analyze kinetic binding data as experimental conditions approach the ligand depletion regime. By comparing the results

SUBMITTER: McNeely PM 

PROVIDER: S-EPMC5896570 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature