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Technology combination to address GPCR allosteric modulator drug-discovery pitfalls.

Schann S, Bouvier M, Neuville P

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.

Drug Discov Today Technol 2013;10(2):e261-7.

Pubmed ID: 24050277

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