Related Experiment Video
Updated: Jun 5, 2026

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
Seeking Ligand Bias: Assessing GPCR Coupling to Beta-Arrestins for Drug Discovery
Laura M Bohn1, Patricia H McDonald
1Departments of Molecular Therapeutics and Neuroscience, The Scripps Research Institute, 130 Scripps Way #2A2, Jupiter, FL 33458, lbohn@scripps.edu.
Abstract:
G protein-coupled receptors (GPCR) are the major site of action for endogenous hormones and neurotransmitters. Early drug discovery efforts focused on determining whether ligands could engage G protein coupling and subsequently activate or inhibit cognate "second messengers." Gone are those simple days as we now realize that receptors can also couple βarrestins. As we delve into the complexity of ligand-directed signaling and receptosome scaffolds, we are faced with what may seem like endless possibilities triggered by receptor-ligand mediated events.
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