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PET Imaging of Estrogen Receptors Using 18F-Based Radioligands

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Estrogen Receptors

Part of the book series: Methods in Molecular Biology ((MIMB,volume 2418))

Abstract

In vivo molecular imaging of estrogen receptor alpha (ER) can be performed via positron emission tomography (PET) using ER-specific radioligands, such as 16α-[18F]fluoro-17β-estradiol (18F-FES). 18F-FES is a radiopharmaceutical recently approved by the United States Food and Drug Administration for use with PET imaging to detect ER+ lesions in patients with recurrent or metastatic breast cancer as an adjunct to biopsy. 18F-FES PET imaging has been used in clinical studies and preclinical research to assess whole-body ER protein expression and ligand binding function across multiple metastatic sites, to demonstrate inter-tumoral and temporal heterogeneity of ER expression, to quantify the pharmacodynamic effects of ER antagonist treatment, and to predict endocrine therapy response. 18F-FES PET has also been studied for imaging ER in endometrial and ovarian cancer. This chapter details the experimental protocol for 18F-FES PET imaging of ER in preclinical tumor xenograft models. Consistent adherence to key methodologic details will facilitate obtaining meaningful and reproducible 18F-FES PET preclinical imaging results, which could yield additional insight for clinical trials regarding imaging biomarkers and oncologic therapy.

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Acknowledgments

The authors acknowledge the University of Wisconsin-Madison Cyclotron Laboratory for 18F production, the Radiopharmaceutical Production Facility for 18F-FES synthesis, and the University of Wisconsin Small Animal Imaging & Radiotherapy Facility (Cancer Center Support Grant: NCI P30 CA014520), including Ashley Weichmann, for small animal PET/CT scanning. We also thank the Translational Research Initiatives in Pathology laboratory, in part supported by the Department of Pathology and Laboratory Medicine and the University of Wisconsin Carbone Cancer Center Support Grant (P30 CA014520) and the Experimental Pathology Laboratory (P30 CA014520) for histology services. We are also grateful to Dr. John Katzenellenbogen for his helpful comments regarding the manuscript.

Research support for 18F-FES PET/CT small animal imaging experiments include the Philips Healthcare/Radiological Society of North America Research Seed Grant, American Cancer Society Institutional Research Grant Pilot Award, Mary Kay Innovative/Translational Cancer Research Grant, University of Wisconsin Department of Radiology, and the University of Wisconsin Carbone Cancer Center Support Grant P30 CA014520.

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  1. Manoj Kumar

    Present address: Department of Radiology, Canary Center at Stanford for Cancer Early Detection, Stanford School of Medicine, Palo Alto, CA, USA

Authors and Affiliations

  1. Department of Radiology, University of Wisconsin School of Medicine and Public Health, Madison, WI, USA

    Manoj Kumar, Kelley Salem & Amy M. Fowler

  2. University of Wisconsin Carbone Cancer Center, Madison, WI, USA

    Justin J. Jeffery & Amy M. Fowler

  3. Department of Medical Physics, University of Wisconsin School of Medicine and Public Health, Madison, WI, USA

    Amy M. Fowler

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  1. Manoj Kumar
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  2. Kelley Salem
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  4. Amy M. Fowler
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Correspondence to Amy M. Fowler .

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Editors and Affiliations

  1. Sanford School of Medicine, University of South Dakota, Vermillion, SD, USA

    Kathleen M. Eyster

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Kumar, M., Salem, K., Jeffery, J.J., Fowler, A.M. (2022). PET Imaging of Estrogen Receptors Using 18F-Based Radioligands. In: Eyster, K.M. (eds) Estrogen Receptors. Methods in Molecular Biology, vol 2418. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-1920-9_9

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  • DOI: https://doi.org/10.1007/978-1-0716-1920-9_9

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