Technology combination to address GPCR allosteric modulator drug-discovery pitfalls.
Allosteric modulators (AMs) represent a novel paradigm to therapeutically target G-protein-coupled receptors (GPCRs). However, their identification and characterization using standard functional assays remain elusive due to the ‘context-dependent phenomena’. Novel technological approaches such as combining a Fluorescence Resonance Energy Transfer (FRET)-based library filtering with a Bioluminescence Resonance Energy Transfer (BRET)-based multiparametric compound profiling can circumvent the limitations of current GPCR screening processes and simplify the discovery of biased AMs.
Stephan
S
Schann
Michel
M
Bouvier
Pascal
P
Neuville
D000494:Allosteric Regulation; D015374:Biosensing Techniques; D055808:Drug Discovery; D031541:Fluorescence Resonance Energy Transfer; D008024:Ligands; D008163:Luminescent Measurements; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
D008024:Ligands; D043562:Receptors, G-Protein-Coupled