Targeted functional imaging of estrogen receptors with 99mTc-GAP-EDL

European Journal of Nuclear Medicine and Molecular Imaging
Nobukazu TakahashiE Edmund Kim

Abstract

To evaluate the feasibility of using (99m)Tc-glutamate peptide-estradiol in functional imaging of estrogen receptor-positive [ER(+)] diseases. 3-Aminoethyl estradiol (EDL) was conjugated to glutamate peptide (GAP) to yield GAP-EDL. Cellular uptake studies of (99m)Tc-GAP-EDL were conducted in ER(+) cell lines (MCF-7, 13762 and T47D). To demonstrate whether GAP-EDL increases MAP kinase activation, Western blot analysis of GAP-EDL was performed in 13762 cells. Biodistribution was conducted in nine rats with 13762 breast tumors at 0.5-4 h. Each rat was administered (99m)Tc-GAP-EDL. Two animal models (rats and rabbits) were created to ascertain whether tumor uptake of (99m)Tc-GAP-EDL was via an ER-mediated process. In the tumor model, breast tumor-bearing rats were pretreated with diethylstilbestrol (DES) 1 h prior to receiving (99m)Tc-GAP-EDL. In the endometriosis model, part of the rabbit uterine tissue was dissected and grafted to the peritoneal wall. The rabbit was administered with (99m)Tc-GAP-EDL. There was a 10-40% reduction in uptake of (99m)Tc-GAP-EDL in cells treated with DES or tamoxifen compared with untreated cells. Western blot analysis showed an ERK1/2 phosphorylation process with GAP-EDL. Biodistribution studies show...Continue Reading

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Citations

Apr 4, 2007·European Journal of Nuclear Medicine and Molecular Imaging·Rakesh Kumar
Mar 5, 2009·Molecular Cancer Therapeutics·Ji Yuan WuRazelle Kurzrock
Mar 28, 2013·International Journal of Biomedical Imaging·Qingqing Meng, Zheng Li
Oct 16, 2015·Nuclear Medicine and Biology·Xiaotian XiaXiaoli Lan
Jul 21, 2016·Nuclear Medicine Communications·Hao LiuMei Tian

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