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

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

  • 1Unidade de Ciências Químicas e Radiofarmacêuticas, Instituto Tecnológico e Nuclear, Sacavém, Portugal

    2Centro de Investigação em Meio Ambiente Genética e Oncobiologia (CIMAGO)

    3Faculty of Science, United Arab Emirates University, United Arab Emirates

    4Instituto de Biofísica/Biomatemática, IBILI, FMUC, Coimbra, Portugal

    5Clínica Ginecológica, FMUC, Coimbra, Portugal

*Address correspondence to this author at the Unidade de Ciências Químicas e Radiofarmacêuticas, Instituto Tecnológico e Nuclear, Estrada Nacional 10, 2686-953 Sacavém, Portugal; Tel: 351 219946195; Fax: 351 219946185; E-mail: [email protected]

Received: October 28, 2010 Revised: January 11, 2011 Accepted: July 07, 2011

Current Radiopharmaceuticals 5(2):p 124-141, 2012.

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.

Copyright © 2012Bentham Science Publisher