title: Estrogen receptor ligands for targeting breast tumours: a brief outlook on radioiodination strategies.
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.
authors.affiliation: Unidade de Ciências Químicas e Radiofarmacêuticas, Instituto Tecnológico e Nuclear, Estrada Nacional 10, 2686-953 Sacavém, Portugal. cmelo@itn.pt
authors.forename: Maria Cristina
authors.initials: MC
authors.lastname: Oliveira
authors.forename: Carina
authors.initials: C
authors.lastname: Neto
authors.forename: Lurdes
authors.initials: L
authors.lastname: Gano
authors.forename: Fernanda
authors.initials: F
authors.lastname: Marques
authors.forename: Isabel
authors.initials: I
authors.lastname: Santos
authors.forename: Thies
authors.initials: T
authors.lastname: Thiemann
authors.forename: Ana Cristina
authors.initials: AC
authors.lastname: Santos
authors.forename: Filomena
authors.initials: F
authors.lastname: Botelho
authors.forename: Carlos F
authors.initials: CF
authors.lastname: Oliveira
mesh_terms: D001943:Breast Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism; D055808:Drug Discovery; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes / Q000737:chemistry; D007536:Isomerism; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry; D011960:Receptors, Estrogen / Q000378:metabolism*; D013329:Structure-Activity Relationship; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D007457:Iodine Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D011960:Receptors, Estrogen