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

CGF Dickmann; AF McDonald; N Huynh; A Rigopoulos; Z Liu; N Guo; LD Osellame; MA Gorman; MW Parker; HK Gan; AM Scott; U Ackermann; IJG Burvenich; JM White

Journal article

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

CGF Dickmann, AF McDonald, N Huynh, A Rigopoulos, Z Liu, N Guo, LD Osellame, MA Gorman, MW Parker, HK Gan, AM Scott, U Ackermann, IJG Burvenich, JM White

Chemical Communications | Published : 2023

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.

University of Melbourne Researchers

Michael Gorman Author

Michael Parker Author

Andrew Scott Author

Uwe Ackermann Author

Related Projects (1)

MOLECULAR STRUCTURE ELUCIDATION FACILITY

This project aims to provide state-of-the-art X-ray diffraction instrumentation in a shared research facility. X-ray diffraction is essentia..

Grants

Awarded by NHMRC

Funding Acknowledgements

The authors acknowledge the funding support of the Australian Cancer Research Foundation (ACRF) for the <SUP>19</SUP>F 500 MHZ NMR in the Bio21 Melbourne Magnetic Resonance Platform, the Bio21-WEHI Crystallisation Facility in the Melbourne Protein Characterisation Platform, and nanoPET/MRI imaging equipment. The National Imaging Facility, a National Collaborative Research Infrastructure Strategy (NCRIS) is acknowledged (University of Melbourne, Austin Health, La Trobe-ONJCRI and ONJCRI nodes). A. M. S. was supported by an NHMRC Investigator grant (No. 1177837). M. W. P. is an NHMRC Leadership Fellow (APP1194263). This research was undertaken in part using the MX2 beamline at the Australian Synchrotron, part of ANSTO, and made use of the ACRF detector.