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Radioiodinated estradiol dimer for estrogen receptor targeted breast cancer imaging
Author(s) -
Xu Duo,
Peng Chenyu,
Gao Fei,
Guo Zhide,
Zhuang Rongqiang,
Su Xinhui,
Zhang Xianzhong
Publication year - 2020
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13754
Subject(s) - fulvestrant , estrogen receptor , biodistribution , chemistry , estrogen , breast cancer , in vitro , spect imaging , progesterone receptor , cancer research , cancer , nuclear medicine , medicine , biochemistry
The aim of this study was to develop a 1‐(2‐(2‐(2‐(1,2,3‐triazol)ethoxy)ethoxy)ethyl)‐5‐[ 125/131 I]iodo‐1,2,3‐triazole‐diestradiol ([ 125/131 I]ITE2), for estrogen receptor (ER)‐expressing breast cancer imaging with single‐photon emission computed tomography (SPECT). [ 125/131 I]ITE2 was prepared in good radiochemical yield (94.4 ± 0.4%) with high radiochemical purity (>99%). [ 125/131 I]ITE2 had good stability in vitro and moderate molar activity (0.3 ± 0.2 GBq/µmol). Higher uptake in ER‐positive MCF‐7 cells than that of ER‐negative MDA‐MB‐231 cells was observed at all time points. Rats biodistribution showed that [ 131 I]ITE2 had high uptake in ER‐abundant uterine and ovarian (5.7 ± 0.4 and 10.1 ± 1.4%ID/g at 1 hr postinjection) and could be blocked by co‐injection of estradiol (2.7 ± 0.1 and 5.5 ± 0.4%ID/g) obviously. In the SPECT/CT imaging study, [ 125 I]ITE2 showed significant higher uptake in MCF‐7 tumor (3.1 ± 0.4%ID/g) than that of MDA‐MB‐231 (0.9 ± 0.1%ID/g). Furthermore, the specific uptake of [ 125 I]ITE2 in ER‐positive MCF‐7 tumor could be blocked effectively by preadministration of fulvestrant (1.2 ± 0.4%ID/g). A novel radioiodinated dimeric estrogen was designed and synthesized with promising ER targeting ability and specificity. It is worthy of further investigation to validate the advantages of the dimer in ER‐positive breast cancer diagnosis.