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Caspase-3 probes for PET imaging of apoptotic tumor response to anticancer therapy

Filipe Elvas1, Tom Vanden Berghe, Yves Adriaenssens

  • 1Molecular Imaging Center Antwerp, University of Antwerp, 2610 Wilrijk, Belgium. filipe.elvas@uantwerpen.be.

Organic & Biomolecular Chemistry
|April 30, 2019
PubMed

Insights

Researchers developed a new PET imaging probe, [18F]MICA-302, to detect apoptosis by targeting active caspase-3. This tool could help assess anticancer therapy effectiveness non-invasively in patients.

Area of Science:

  • Molecular Imaging
  • Oncology
  • Biochemistry

Background:

  • Apoptosis is crucial for development and homeostasis, and its induction is a key goal in cancer therapy.
  • Caspase activation, particularly caspase-3 and -7, is a central event in apoptosis and a potential biomarker for treatment response.
  • Non-invasive in vivo imaging of apoptosis can enable early assessment of therapeutic efficacy and drug development.

Purpose of the Study:

  • To develop and evaluate novel fluorine-18-labeled caspase-3 activity-based probes (ABPs) for Positron Emission Tomography (PET) imaging of apoptosis.
  • To identify a suitable ABP with high affinity for caspase-3 and favorable properties for in vivo imaging.
  • To assess the potential of the developed radiotracer for monitoring response to anticancer therapy.

Main Methods:

  • Screening of fluorine-19-labeled DEVD peptides with different electrophilic warheads to identify high-affinity ABPs.
  • Radiolabeling of the lead compound with fluorine-18 to create the PET tracer [18F]MICA-302.
  • In vitro evaluation of [18F]MICA-302 for caspase-3 labeling and pharmacokinetic profiling.
  • In vivo microPET imaging in colorectal tumor xenografts to assess tumor accumulation in response to drug treatment.

Main Results:

  • An acyloxymethyl ketone-containing DEVD peptide was identified with low nanomolar affinity for caspase-3.
  • [18F]MICA-302 demonstrated effective labeling of active caspase-3 in vitro and favorable pharmacokinetic properties.
  • μPET imaging revealed increased tumor accumulation of [18F]MICA-302 in drug-treated tumor xenografts compared to controls.

Conclusions:

  • The developed fluorine-18-labeled ABP, [18F]MICA-302, shows promise for PET imaging of apoptosis.
  • This radiotracer may serve as a valuable tool for non-invasive, in vivo assessment of response to anticancer therapies.
  • Further clinical evaluation is warranted to establish its utility in patient management and drug development.

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