Radiopharmacologist's and Radiochemist's View on Targeting the Eph/Ephrin Receptor Tyrosine Kinase System

Christin Neuber1, Birgit Belter1, Constantin Mamat2,3

  • 1Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, Department of Radiopharmaceutical and Chemical Biology, 01328 Dresden, Germany.

ACS Omega
|July 21, 2020
PubMed

Insights

Researchers are developing radiotracers targeting the Eph/ephrin receptor tyrosine kinase family for molecular imaging and therapy. This review covers antibody, peptide, and small molecule approaches for diagnostic applications using positron emission tomography.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Radiopharmaceutical Chemistry

Background:

  • The Eph/ephrin receptor tyrosine kinase family is a target for diagnostics and therapeutics.
  • Extensive efforts have focused on developing drugs targeting extracellular or intracellular domains.
  • Radiopharmaceutical approaches are emerging for molecular imaging and functional characterization.

Purpose of the Study:

  • To review different strategies for developing Eph-targeting radiotracers.
  • To discuss the radiopharmacological characterization of these tracers.
  • To explore applications in molecular imaging, particularly positron emission tomography.

Main Methods:

  • Review of literature on radiotracer development for Eph/ephrin family.
  • Categorization of approaches: antibodies, peptides, and small molecules.
  • Discussion of radiolabeling strategies and synthesis of nonradioactive compounds.

Main Results:

  • Antibodies, peptides, and small molecules are being investigated as Eph-targeting radiotracers.
  • Positron emission tomography (PET) is a key imaging modality.
  • Radiopharmacological characterization is crucial for diagnostic and therapeutic potential.

Conclusions:

  • Various molecular probes are under development for Eph/ephrin-targeted imaging.
  • Small molecules offer promising avenues for radiotracer design and synthesis.
  • Further research is needed to optimize radiotracers for clinical applications.

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