Bromodomain and extraterminal protein-targeted probe enables tumour visualisation in vivo using positron emission

Catherine G Fitzgerald Dickmann1,2,3, Alexander F McDonald2,3, Nhi Huynh3

  • 1Bio21 Institute, The University of Melbourne, Parkville, VIC 3010, Australia. whitejm@unimelb.edu.au.

Chemical Communications (Cambridge, England)
|February 22, 2023
PubMed

Insights

Researchers developed a new fluorine-18 radiolabeled molecule, [18F]BiPET-2, for molecular imaging of Bromodomain and Extraterminal (BET) proteins. This novel tracer shows promise for glioblastoma research and cancer imaging applications.

Area of Science:

  • Oncology
  • Molecular Imaging
  • Epigenetics

Background:

  • Bromodomain and extraterminal (BET) proteins are epigenetic regulators implicated in cancer.
  • BET proteins are promising oncology drug targets.
  • Molecular imaging of BET proteins in cancer has not been achieved.

Purpose of the Study:

  • To develop a novel positron-emitting tracer for molecular imaging of BET proteins.
  • To evaluate the in vitro and preclinical efficacy of the novel tracer in glioblastoma models.

Main Methods:

  • Development of a novel molecule radiolabeled with fluorine-18 ([18F]BiPET-2).
  • In vitro characterization of [18F]BiPET-2.
  • Preclinical evaluation of [18F]BiPET-2 in glioblastoma models.

Main Results:

  • Successful development of [18F]BiPET-2, a novel fluorine-18 radiolabeled molecule.
  • Demonstrated in vitro properties of [18F]BiPET-2.
  • Showcased preclinical efficacy of [18F]BiPET-2 in glioblastoma models.

Conclusions:

  • [18F]BiPET-2 represents a novel molecular imaging tracer targeting BET proteins.
  • This tracer holds potential for advancing glioblastoma research and cancer imaging.