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Current Radiopharmaceuticals


ISSN (Print): 1874-4710
ISSN (Online): 1874-4729

Estrogen Receptor Ligands for Targeting Breast Tumours: A Brief Outlook on Radioiodination Strategies

Author(s): Maria Cristina Oliveira, Carina Neto, Lurdes Gano, Fernanda Marques, Isabel Santos, Thies Thiemann, Ana Cristina Santos, Filomena Botelho and Carlos F. Oliveira

Volume 5, Issue 2, 2012

Page: [124 - 141] Pages: 18

DOI: 10.2174/1874471011205020124

Price: $65


The design and development of radiolabelled estradiol derivatives has been an important area of research due to their recognized value in breast cancer management. The estrogen receptor (ER) is a relevant biomarker in the diagnosis, prognosis and prediction of the therapeutic response in estrogen receptor positive breast tumours. Hence, many radioligands based on estradiol derivatives have been proposed for targeted functional ER imaging. The main focus of this review is to survey the current knowledge on estradiol-based radioiodinated receptor ligands synthesis for breast tumour functional imaging. The main preclinical and clinical achievements in the field will also be briefly presented to make the manuscript more comprehensive.

Keywords: Breast cancer, tumor targeting, SPECT, radioiodination, estrogen receptor, estradiol, Nucleophilic Substitution, SAR

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