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Related Experiment Video

Updated: Jul 4, 2026

High-throughput Functional Screening using a Homemade Dual-glow Luciferase Assay

High-throughput Functional Screening using a Homemade Dual-glow Luciferase Assay

Published on: June 1, 2014

Imaging CXCR4 signaling with firefly luciferase complementation.

Kathryn E Luker¹, Mudit Gupta, Gary D Luker

¹Center for Molecular Imaging, Department of Radiology, University of Michigan Medical School, Ann Arbor, Michigan 48109, USA.

Analytical Chemistry

|June 7, 2008

Summary

Researchers developed a novel imaging reporter to track CXCR4 chemokine receptor activity in cancer. This tool visualizes receptor signaling in vivo, aiding the development of targeted therapies for improved patient survival.

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Last Updated: Jul 4, 2026

High-throughput Functional Screening using a Homemade Dual-glow Luciferase Assay

High-throughput Functional Screening using a Homemade Dual-glow Luciferase Assay

Published on: June 1, 2014

A Cre-Lox P Recombination Approach for the Detection of Cell Fusion In Vivo

A Cre-Lox P Recombination Approach for the Detection of Cell Fusion In Vivo

Published on: January 4, 2012

A Multiplexed Luciferase-based Screening Platform for Interrogating Cancer-associated Signal Transduction in Cultured Cells

A Multiplexed Luciferase-based Screening Platform for Interrogating Cancer-associated Signal Transduction in Cultured Cells

Published on: July 3, 2013

Area of Science:

Oncology
Molecular Imaging
Cell Signaling

Background:

Chemokines and receptors regulate cell functions, and cancer cells exploit this signaling for growth and metastasis.
Understanding in vivo chemokine receptor signaling in cancer is crucial for developing effective therapies.

Purpose of the Study:

To develop a molecular imaging reporter for investigating CXCR4 (C-X-C chemokine receptor type 4) activation in cancer.
To enable in vivo monitoring of CXCR4 signaling dynamics and therapeutic inhibition.

Main Methods:

Developed a firefly luciferase-based protein fragment complementation assay to detect CXCR4 and beta-arrestin interactions.
Validated the reporter system in cell-based assays with CXCL12 (C-X-C chemokine ligand 12) stimulation.
Utilized the reporter for in vivo imaging of CXCR4 activation and inhibition in mouse models.

Main Results:

Demonstrated dose-dependent increases in bioluminescence (>7-fold) upon CXCL12 stimulation, indicating reporter activation.
Confirmed reporter activation is specific and can be blocked by CXCR4 inhibitors.
Successfully visualized CXCR4 signaling and its inhibition in living mice.

Conclusions:

Established a novel, functional imaging reporter for probing CXCR4 signaling in cancer.
The reporter system provides a valuable tool for studying molecular regulation in primary and metastatic cancers.
This technology can advance the development of targeted therapies for cancers driven by CXCR4 signaling.