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Updated: May 17, 2025

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
Intracellular GPCR modulators enable precision pharmacology
Brian E Krumm1, Bryan L Roth1,2
1Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC USA.
Abstract:
G-protein-coupled receptors (GPCRs) have proven to be the most successful target class for drug discovery but their complicated signal transduction pathways cause difficulties for drug development. Recently, ligands have been identified that engage an intracellular binding site which promotes pathway biased signal in cooperation with orthosteric ligands. Here, we explore the topic of biased signaling and intracellular modulators to understand their application for precision pharmacology of Class A or Rhodopsin-Like GPCRs.
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