Targeted Molecular Radiotherapy of Estrogen Receptor Postive Tumors. Report for June 25, 2005 to March 26, 2006

摘要

The overall objectives of the proposal were to develop estrogen receptor (ER) binding small molecule radiopharmaceuticals for targeted radiotherapy of ER positive (ER+) tumors. In particular, this proposal focused on embedding a 186/188Re or a 32P radionuclide into an estrogen steroidal framework by isosteric substitution such that the resulting structure is topologically similar to the estrogen (estrogen mimic). The estrogen mimic molecules expected to bind to the ER and exhibit biodistribution akin to that of native estrogen due to structural mimicry. It is anticipated that the 186,188Re- or a 32P-containing estrogen mimics will be useful for targeted molecular radiotherapy of ER+ tumors.