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

Catherine G Fitzgerald Dickmann; Alexander F McDonald; Nhi Huynh; Angela Rigopoulos; Zhanqi Liu; Nancy Guo; Laura D Osellame; Michael A Gorman; Michael W Parker; Hui K Gan; Andrew M Scott; Uwe Ackermann; Ingrid J G Burvenich; Jonathan M White

doi:10.1039/d2cc04813b

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

Chem Commun (Camb). 2023 Mar 9;59(21):3126-3129. doi: 10.1039/d2cc04813b.

Authors

Catherine G Fitzgerald Dickmann^{1

2

3}, Alexander F McDonald^{2

3}, Nhi Huynh³, Angela Rigopoulos³, Zhanqi Liu³, Nancy Guo³, Laura D Osellame³, Michael A Gorman¹, Michael W Parker^{1

4

5}, Hui K Gan², Andrew M Scott^{2

3

6}, Uwe Ackermann^{2

3}, Ingrid J G Burvenich², Jonathan M White¹

Affiliations

¹ Bio21 Institute, The University of Melbourne, Parkville, VIC 3010, Australia. whitejm@unimelb.edu.au.
² Tumour Targeting Laboratory, Olivia Newton-John Cancer Research Institute, and School of Cancer Medicine, La Trobe University, Heidelberg, Australia. uwea@unimelb.edu.au.
³ Department of Molecular Imaging and Therapy, Austin Hospital, Heidelberg, Australia.
⁴ ACRF Facility for Innovative Cancer Drug Discovery, Bio21 Institute, The University of Melbourne, Parkville, VIC 3010, Australia.
⁵ ACRF Rational Drug Discovery Centre, St. Vincent's Institute of Medical Research, VIC 3065, Australia.
⁶ Faculty of Medicine, University of Melbourne, Parkville, Australia.

PMID: 36809538
DOI: 10.1039/d2cc04813b

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.

MeSH terms

Glioblastoma* / diagnostic imaging
Humans
Positron-Emission Tomography / methods
Protein Domains
Proteins*

Substances

Proteins