Related Experiment Video

Updated: Jan 31, 2026

Deciphering the Structural Effects of Activating EGFR Somatic Mutations with Molecular Dynamics Simulation
15:05

Deciphering the Structural Effects of Activating EGFR Somatic Mutations with Molecular Dynamics Simulation

Published on: May 20, 2020

9.3K

Real-time molecular optical micro-imaging of EGFR mutations using a fluorescent erlotinib based tracer

Maxime Patout1,2,3, Florian Guisier4,5, Xavier Brune6

  • 1Rouen University Hospital, Clinique Pneumologique & CIC INSERM U 1404, F-76000, Rouen, France. maxime.patout@chu-rouen.fr.

BMC Pulmonary Medicine
|January 8, 2019
PubMed
Abstract

Insights

A novel fluorescent erlotinib tracer successfully identified epidermal growth factor receptor (EGFR) mutations in lung adenocarcinoma tumors. This theranostic agent shows promise for molecular imaging of EGFR-mutated cancers.

Area of Science:

  • Oncology
  • Molecular Imaging
  • Biochemistry

Background:

  • Epidermal growth factor receptor (EGFR) mutations are key targets in lung adenocarcinoma.
  • Current methods for detecting EGFR mutations involve tumoral DNA sequencing.
  • A need exists for advanced imaging techniques to identify EGFR-mutated tumors.

Purpose of the Study:

  • To evaluate a novel fluorescent-labeled erlotinib theranostic agent.
  • To assess its utility for molecular imaging of EGFR-mutated tumors.
  • To perform in vitro and ex vivo imaging using a mice xenograft model and fibred confocal fluorescence microscopy (FCFM).

Main Methods:

  • Synthesized a fluorescent tracer by conjugating fluorescein to erlotinib.
  • Xenografted human adenocarcinoma cell lines (mutated and wild-type EGFR) onto nude mice.
  • Performed MTT viability assays, in vitro, and ex vivo FCFM imaging, recording median fluorescence intensity (MFI).

Main Results:

  • The fluorescent tracer retained erlotinib's cytotoxic properties.
  • In vitro FCFM imaging distinguished mutated EGFR cell lines from wild-type (p < 0.001).
  • Ex vivo imaging showed significantly higher MFI in mutated EGFR xenografts (p < 0.001), with 100% sensitivity and 96.3% specificity.

Conclusions:

  • Real-time molecular imaging with fluorescent erlotinib effectively identifies EGFR mutations in tumors.
  • This theranostic approach offers a promising tool for diagnosing EGFR-mutated lung adenocarcinoma.
  • The study demonstrates the potential of fluorescent erlotinib for ex vivo tumor identification.
Keywords:
EGFREpidermal growth factorErlotinibFibred confocal fluorescence microscopyLung cancerMolecular imagingTheranostic

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