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

Maria      Cristina Oliveira; Carina      Neto; Lurdes      Gano; Fernanda      Marques; Isabel      Santos; Thies      Thiemann; Ana      Cristina Santos; Filomena      Botelho; Carlos      F. Oliveira

Abstract

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