PET Imaging of FSHR Expression in Tumors with (68)Ga-Labeled FSH1 Peptide.
PET Imaging of FSHR Expression in Tumors with (68)Ga-Labeled FSH1 Peptide.
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使用 68Ga 标记的 FSH1 肽对肿瘤中 FSHR 表达进行 PET 成像
DOI：
10.1155/2017/2674502
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发表时间：
2017
影响因子：
--
通讯作者：
Yang M
中科院分区：
文献类型：
--
作者：
Pan D;Liu G;Xu Y;Wang Y;Yue Y;Wang L;Yan J;Wang X;Yang R;Yang M
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.
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影响因子：
4.7
作者：
Lang, Lixin;Li, Weihua;Guo, Ning;Ma, Ying;Zhu, Lei;Kiesewetter, Dale O.;Shen, Baozhong;Niu, Gang;Chen, Xiaoyuan
通讯作者：
Chen, Xiaoyuan
影响因子：
12.4
作者：
Kiesewetter DO;Guo N;Guo J;Gao H;Zhu L;Ma Y;Niu G;Chen X
通讯作者：
Chen X
DOI：
10.1007/s00259-007-0658-0
发表时间：
2008-05
影响因子：
9.1
作者：
Kramer-Marek, Gabriela;Kiesewetter, Dale O.;Martiniova, Lucia;Jagoda, Elaine;Lee, Sang Bong;Capala, Jacek
通讯作者：
Capala, Jacek
影响因子：
14
作者：
Yang D;Feng L;Dougherty CA;Luker KE;Chen D;Cauble MA;Banaszak Holl MM;Luker GD;Ross BD;Liu Z;Hong H
通讯作者：
Hong H
影响因子：
4.9
作者：
Hong H;Yan Y;Shi S;Graves SA;Krasteva LK;Nickles RJ;Yang M;Cai W
通讯作者：
Cai W