The presence and activity of steroid receptors such as the progesterone receptor (PR), is an important diagnostic and prognostic marker for hormone dependent cancers: namely breast, uterine, and ovarian. Determination of receptor status can inform physicians of the progression of a tumor as well as identify treatment options. The loss of PR expression correlates to more aggressive phenotypes. Immunohistochemical assays are currently used to measure receptor status but require tissue biopsy. Therefore, the development of a noninvasive imaging technique that would determine receptor status would have significant impact on early detection and costs. Magnetic resonance imaging (MRI) techniques can perform longitudinal studies by allowing a series of measurements to be conducted over time. Our research has focused on the development of PR-targeted MR probes to detect the progesterone receptor status in vivo (Figure 1) . Optimization of our previously reported agents has successfully led to contrast agents with increased water solubility, retention of receptor binding affinity and PR activation, and preferential accumulation in tissues that up-regulate PR. ??

Design and synthesis of a series of progesterone receptor-targeted MR imaging probes

247th National Meeting (2014)

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