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.
Abstract:
Bromodomain and extraterminal (BET) proteins, a family of epigenetic regulators, have emerged as important oncology drug targets. BET proteins have not been targeted for molecular imaging of cancer. Here, we report the development of a novel molecule radiolabelled with positron emitting fluorine-18, [18F]BiPET-2, and its in vitro and preclinical evaluation in glioblastoma models.
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.
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