Luminogenic HiBiT Peptide-Based NanoBRET Ligand Binding Assays for Melatonin Receptors.

ABSTRACT: The two human melatonin receptors MT₁ and MT₂, which belong to the G protein-coupled receptor (GPCR) family, are important drug targets with approved indications for circadian rhythm- and sleep-related disorders and major depression. Currently, most of the pharmacological studies were performed using [³H]melatonin and 2-[¹²⁵I]iodomelatonin (2-[¹²⁵I]-MLT) radioligands. Recently, NanoLuc-based bioluminescence resonance energy transfer (NanoBRET) monitoring competitive binding between fluorescent tracers and unmodified test compounds has emerged as a sensitive, nonradioactive alternative for quantifying GPCR ligand engagement on the surface of living cells in equilibrium and real time. However, developing such assays for the two melatonin

SUBMITTER: Gbahou F 

PROVIDER: S-EPMC9380205 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature