PET Imaging of FSHR Expression in Tumors with 68Ga-Labeled FSH1 Peptide
PET Imaging of FSHR Expression in Tumors with 68Ga-Labeled FSH1 Peptide
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DOI：
10.1155/2017/2674502
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发表时间：
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影响因子：
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通讯作者：
Min Yang
中科院分区：
文献类型：
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作者：
Donghui Pan;Guifeng Liu;Yuping Xu;Yanting Wang;Yuanyuan Yue;Lizhen Wang;Junjie Yan;Xinyu Wang;Runlin Yang;Min Yang
FSHR is an appealing target for cancer theranostics. Radiolabeled FSH1 and its derivatives have shown potential to in vivo detect.FSHR expression. However, moderate labeling yields (∼50% nondecay-corrected) may partially limit their wide use. 68Ga is an.excellent PET nuclide due to availability, nearly quantitative reaction, and short physical half-life. In this study, 68Ga labeled FSH1.peptide was developed for imaging of FSHR in cancers. In vitro studies and MicroPET imaging were performed in PC-3 prostate.tumor model. [68Ga] Ga-NOTA-MAL-FSH1 can be produced within 20 min with 93.2 ± 2.1% yield and the radiochemical purity.was greater than 95%. It showed that [68Ga] Ga-NOTA-MAL-FSH1 possessed FSHR binding affinities.The tracer was stable in PBS.and human serum for at least 2 hours. MicroPET imaging revealed that the PC-3 xenografts were clearly visualized and the tumor.uptakes were 1.87±0.10, 1.26±0.06, and 0.71±0.10%ID/g at 0.5, 1 h, and 2 h postinjection.The corresponding tumor to blood and.tumor to muscle ratios were 1.77 ± 0.70, 7.94 ± 1.35, and 10.37 ± 1.16 and 7.42 ± 0.46, 26.13 ± 2.99, and 36.40 ± 2.54, respectively..FSHR binding specificity was also demonstrated by reduced tumor uptake of [68Ga] Ga-NOTA-MAL-FSH1 after coinjecting excess.unlabeled FSH1 peptide.The favorable characters of [68Ga] Ga-NOTA-MAL-FSH1 such as convenient synthesis and specific tumor.uptake warrant its further investigation for FSHR expression imaging.
