PDF herunterladen
Open Access
CC BY 4.0 · World J Nucl Med 2024; 23(03): 153-160
DOI: 10.1055/s-0044-1786518
Original Article

Characterization of an Estrogen Receptor α-Selective 18F-Estradiol PET Tracer

Autoren

  • Pavel Sluka

    1   Eastern Health Clinical School, Monash University, Box Hill, VIC, Australia

  • Uwe Ackermann

    2   Department of Molecular Imaging and Therapy, Austin Hospital, Heidelberg, VIC, Australia
    3   Olivia Newton-John Cancer Research Institute, Heidelberg, VIC, Australia
    4   School of Cancer Medicine, La Trobe University, Bundoora, VIC, Australia
    5   The University of Melbourne, Parkville, VIC, Australia

  • Angela Rigopoulos 

    3   Olivia Newton-John Cancer Research Institute, Heidelberg, VIC, Australia
    4   School of Cancer Medicine, La Trobe University, Bundoora, VIC, Australia

  • Hady Wardan

    1   Eastern Health Clinical School, Monash University, Box Hill, VIC, Australia

  • Carmel Pezaro

    1   Eastern Health Clinical School, Monash University, Box Hill, VIC, Australia
    6   Department of Oncology, Eastern Health, Box Hill, VIC, Australia

  • Ingrid J.G. Burvenich 

    3   Olivia Newton-John Cancer Research Institute, Heidelberg, VIC, Australia
    4   School of Cancer Medicine, La Trobe University, Bundoora, VIC, Australia

  • Andrew M. Scott

    2   Department of Molecular Imaging and Therapy, Austin Hospital, Heidelberg, VIC, Australia
    3   Olivia Newton-John Cancer Research Institute, Heidelberg, VIC, Australia
    4   School of Cancer Medicine, La Trobe University, Bundoora, VIC, Australia
    5   The University of Melbourne, Parkville, VIC, Australia

  • Ian D. Davis

    1   Eastern Health Clinical School, Monash University, Box Hill, VIC, Australia
    6   Department of Oncology, Eastern Health, Box Hill, VIC, Australia

Funding This work was supported, in part, by funds from the Eastern Health Foundation Linda Williams Memorial Oncology Research Grant (EHFRG2017_079), a Prostate Cancer Foundation of Australia New Directions Development Award (NDDA1311), the Operational Infrastructure Support Program provided by the Victorian Government, Australia, and the Australian Cancer Research Foundation. IDD was supported by an NHMRC Practitioner Fellowship (APP1102604). AMS is supported by an NHMRC Practitioner Fellowship (APP1084178) and Investigator Grant (APP1199837).
Weitere Informationen
Auch verfügbar auf
  Lizenzen und Reprints

Abstract

Objective Conventional imaging of cancer with modalities such as computed tomography or magnetic resonance imaging provides little information about the underlying biology of the cancer and consequently little guidance for systemic treatment choices. Accurate identification of aggressive cancers or those that are likely to respond to specific treatment regimens would allow more precisely tailored treatments to be used. The expression of the estrogen receptor α subunit is associated with a more aggressive phenotype, with a greater propensity to metastasize. We aimed to characterize the binding properties of an 18F-estradiol positron emission tomography (PET) tracer in its ability to bind to the α and β forms of estrogen receptors in vitro and confirmed its binding to estrogen receptor α in vivo.

Methods The 18F-estradiol PET tracer was synthesized and its quality confirmed by high-performance liquid chromatography. Binding of the tracer was assessed in vitro by saturation and competitive binding studies to HEK293T cells transfected with estrogen receptor α (ESR1) and/or estrogen receptor β (ESR2). Binding of the tracer to estrogen receptor α in vivo was assessed by imaging of uptake of the tracer into MCF7 xenografts in BALB/c nu/nu mice.

Results The 18F-estradiol PET tracer bound with high affinity (94 nM) to estrogen receptor α, with negligible binding to estrogen receptor β. Uptake of the tracer was observed in MCF7 xenografts, which almost exclusively express estrogen receptor α.

Conclusion 18F-estradiol PET tracer binds in vitro with high specificity to the estrogen receptor α isoform, with minimal binding to estrogen receptor β. This may help distinguish human cancers with biological dependence on estrogen receptor subtypes.

Keywords

estrogen receptor α - estrogen receptor β - positron emission tomography - radiopharmaceuticals - competitive binding

Supplementary Material



Publikationsverlauf

Artikel online veröffentlicht:
18. Juni 2024

© 2024. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting unrestricted use, distribution, and reproduction so long as the original work is properly cited. (https://creativecommons.org/licenses/by/4.0/)

Thieme Medical and Scientific Publishers Pvt. Ltd.
A-12, 2nd Floor, Sector 2, Noida-201301 UP, India