Abstract

It has now been more than 30 years since the laboratory verification of the localization of estrogen in certain animal tissues. Much has been learned since that time regarding the details of this process, including the presence of specific receptors for these hormones in target tissues, the mechanism of ligand binding, the association of the ligand-receptor complex with unique chromatin sequences, and the activation of transcription. A concrete use of this knowledge has been the exploitation of these receptors as a targeting mechanisms for radiopharmaceuticals. This is an exciting area that encompasses both diagnosis and therapy. This review will summarize the in vitro and in vivo data obtained from evaluation of the many compounds that have been examined as radiolabeled receptor ligands, and will also discuss the chemistry necessary for their preparation. In particular, relative binding affinity values for relevant compounds will be tabulated, grouped according to molecular class. For those materials for which biodistributions have been performed, uterine (target), liver (nontarget, clearance), and, when available, tumor tissue uptake values are presented. These data should provide a reminder of what has been accomplished, and should serve as a working reference for those engaged in the pursuit of new candidates for these applications.