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Updated: Apr 14, 2026

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
Accelerating GPCR drug discovery through computation and experiment integrated with direct detection of ligand
Judith Su1, Stephen B Liggett2, Soo-Kyung Kim3
1Wyant College of Optical Sciences and Department of Biomedical Engineering, The University of Arizona, Arizona, USA.
Abstract:
We present a perspective on an integrated workflow for GPCR drug discovery that combines computational modeling, functional cellular assays, and FLOWER, a label-free ultra-sensitive optical biosensing system for quantitating direct ligand receptor binding. We use bitter and sweet taste receptors (TAS2Rs and T1R2/T1R3) as examples of how FLOWER resolves receptor activation mechanisms left ambiguous after in silico screening and cell assays. This workflow offers a generalizable strategy for accelerating the discovery of selective and mechanism informed GPCR targeting therapeutics.
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