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Bioorthogonally Applicable Fluorescence Deactivation Strategy for Receptor Kinetics Study and Theranostic

Steffen van der Wal1, Clarize M de Korne1, Laurens G L Sand2,3

  • 1Interventional Molecular Imaging Laboratory, Department of Radiology, Leiden University Medical Center, Albinusdreef 2, 2333 ZA, Leiden, The Netherlands.

Chembiochem : a European Journal of Chemical Biology
|June 5, 2018
PubMed

Insights

A novel deactivatable fluorescence-quenching method effectively assesses receptor availability for theranostic pretargeting. This approach enables straightforward screening of membrane receptors for theranostic applications.

Area of Science:

  • Molecular Imaging
  • Bioconjugation Chemistry
  • Theranostics

Background:

  • Theranostic pretargeting requires efficient methods to assess receptor availability.
  • Distinguishing between cell-surface and internalized receptors is crucial for targeted therapies.
  • Click chemistry offers versatile tools for bioconjugation and molecular imaging.

Purpose of the Study:

  • To develop and validate a click-chemistry-based deactivatable fluorescence-quenching concept for assessing receptor availability.
  • To evaluate the efficacy of this approach in a cell-based model using chemokine receptor CXCR4.
  • To demonstrate the potential for screening membrane receptors for theranostic applications.

Main Methods:

  • A deactivatable tracer (N3-Cy5-AcTZ14011) targeting CXCR4 was synthesized.
  • A quencher dye (Cy7-DBCO) was used to induce fluorescence quenching via click chemistry.
  • Förster Resonance Energy Transfer (FRET) was employed to quantify signal reduction.
  • Cell-based assays were performed to differentiate between membranous and internalized receptor fractions.

Main Results:

  • The deactivatable tracer showed a >90% FRET-based signal reduction within minutes upon quencher addition.
  • The method successfully discriminated between membranous and internalized CXCR4 fractions based on quenching and internalization kinetics.
  • An activatable tracer variant proved unsuccessful in vitro, highlighting the advantages of the deactivatable approach.

Conclusions:

  • The developed deactivatable fluorescence-quenching concept provides a straightforward method for assessing receptor availability.
  • This approach is suitable for screening membrane receptors and evaluating their potential in receptor-(pre-)targeted theranostics.
  • The technique allows for quantitative assessment of receptor localization, crucial for optimizing theranostic strategies.
Keywords:
click chemistrydeactivatablefluorescencepretargetingtheranostics

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