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†

Catherine G. Fitzgerald Dickmann,

^abc Alexander F. McDonald,

^bc Nhi Huynh,^c Angela Rigopoulos,^c Zhanqi Liu,^c Nancy Guo,^c Laura D. Osellame,

^c Michael A. Gorman,

^a Michael W. Parker,

^aef Hui K. Gan,

^b Andrew M. Scott,

^bcd Uwe Ackermann,

*^bc Ingrid J. G. Burvenich

*^b and Jonathan M. White

*^a

Author affiliations

* Corresponding authors

^a Bio21 Institute, The University of Melbourne, Parkville, VIC 3010, Australia
E-mail: whitejm@unimelb.edu.au

^b Tumour Targeting Laboratory, Olivia Newton-John Cancer Research Institute, and School of Cancer Medicine, La Trobe University, Heidelberg, Australia
E-mail: uwea@unimelb.edu.au, Ingrid.burvenich@onjcri.org.au

^c Department of Molecular Imaging and Therapy, Austin Hospital, Heidelberg, Australia

^d Faculty of Medicine, University of Melbourne, Parkville, Australia

^e ACRF Facility for Innovative Cancer Drug Discovery, Bio21 Institute, The University of Melbourne, Parkville, Australia

^f ACRF Rational Drug Discovery Centre, St. Vincent's Institute of Medical Research, Australia

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.

Chemical Communications

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

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

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