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Mol Pharm. 2011 Aug 1;8(4):1390-400. doi: 10.1021/mp200219e. Epub 2011 Jul 8.

A steroid-conjugated magnetic resonance probe enhances contrast in progesterone receptor expressing organs and tumors in vivo.

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Department of Chemistry, Northwestern University, Evanston, Illinois 60208, USA.


Progesterone receptor (PR) is a significant biomarker in diseases such as endometriosis and breast, ovarian, and uterine cancers that is associated with disease prognosis and therapeutic efficacy. While receptor status is currently determined by immunohistochemistry assays, the development of noninvasive PR imaging agents could improve molecular characterization, treatment decisions, and disease monitoring. ProGlo, a progesterone-conjugated magnetic resonance imaging (MRI) contrast agent, was evaluated in vivo to determine whether it targets and enhances signal intensity in organs and tumors that express high PR levels. A tissue distribution study indicated that ProGlo accumulates in the PR-rich uterus, which was confirmed by in vivo imaging studies. Ex vivo images of these organs revealed that ProGlo was distributed in the substructures that express high PR levels. In xenograft tumor models, ProGlo was taken up to a greater extent than the nonfunctionalized Gd-DO3A in tumors, particularly in PR(+) tumors. The ability to accumulate and enhance signal intensity in PR(+) organs and tumors suggests that ProGlo may be a promising MRI probe for PR(+) diseases.

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