1. Radioiodinated Ethinylestradiol Derivatives for Estrogen Receptor Targeting Breast Cancer Imaging
- Author
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Huanhuan Liu, Xiaoru Lin, Duo Xu, Jingchao Li, Jianyang Fang, Jindian Li, Lingxin Meng, Xinying Zeng, Yesen Li, Jinxiong Huang, Zhide Guo, and Xianzhong Zhang
- Subjects
Organic Chemistry ,Drug Discovery ,Biochemistry - Abstract
[Image: see text] Two novel PEGylated ethinylestradiol (PEG = poly(ethylene glycol)) estrogen receptor (ER) targeting probes [(131)I]EITE and [(131)I]MITE were synthesized and evaluated. Both probes had a nanomolar binding affinity to the ER receptor (36.47 nM for [(131)I]EITE and 61.83 nM for [(131)I]MITE). They showed high uptake in ER-positive MCF-7 cells and tumors, which could be significantly blocked by a coinjection of excess estradiol. Their ER specificities were further demonstrated by the low uptake in ER-negative MDA-MB-231 cells and tumors. The maximum tumor-to-muscle (T/M) ratios reach to 6.59 for [(131)I]EITE at 1 h postinjection (p.i.) and to 3.69 for [(131)I]MITE at 2 h p.i. in MCF-7 tumors. Among these two probes, [(131)I]EITE showed a faster tumor accumulation and a higher T/M ratio indicating it could be a better candidate for the potential diagnosis of ER-positive breast cancers.
- Published
- 2021