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April 5, 2026Cancer Research

Adapting A TR-FRET Platform For GPCR Internalization And Recycling Kinetics

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Authors

JGJie GaoAOAn OuyangSCSpencer Chiang

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Overview

Demonstrates a new TR-FRET platform to quantify GPCR internalization and recycling kinetics, suggesting improvements in drug discovery processes.

Key Points

  • The aim is to adapt a TR-FRET platform to monitor the internalization and recycling kinetics of GPCRs in real time.
  • Adaptation of a TR-FRET-based platform to study receptor kinetics.
  • Use of donor-acceptor fluorophore pairs with receptor constructs.
  • Real-time tracking of ligand-induced receptor trafficking in living cells.
  • High TR-FRET signals were observed before internalization, indicating active receptors.
  • TR-FRET signal decreased during receptor internalization and increased upon recycling.
  • The platform facilitates discrimination of biased agonists and profiling of receptor dynamics.

Cite This Study

Gao et al. (2026) studied this question.

synapsesocial.com/papers/69d1fe07a79560c99a0a4833https://doi.org/10.1158/1538-7445.am2026-472
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