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PET Imaging of FSHR Expression in Tumors with Ga-Labeled FSH1 Peptide

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. Ga is an excellent PET nuclide due to availability, nearl... Full description

Journal Title: Contrast Media & Molecular Imaging 2017, Vol.2017, 8 pages
Main Author: Pan, Donghui
Other Authors: Liu, Guifeng , Xu, Yuping , Wang, Yanting , Yue, Yuanyuan , Wang, Lizhen , Yan, Junjie , Wang, Xinyu , Yang, Runlin , Yang, Min
Format: Electronic Article Electronic Article
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ID: ISSN: 1555-4309 ; E-ISSN: 1555-4317 ; DOI: 10.1155/2017/2674502
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recordid: hindawi10.1155/2017/2674502
title: PET Imaging of FSHR Expression in Tumors with Ga-Labeled FSH1 Peptide
format: Article
creator:
  • Pan, Donghui
  • Liu, Guifeng
  • Xu, Yuping
  • Wang, Yanting
  • Yue, Yuanyuan
  • Wang, Lizhen
  • Yan, Junjie
  • Wang, Xinyu
  • Yang, Runlin
  • Yang, Min
subjects:
  • Positron Emission Tomography – Methods
  • Hormone Receptors – Properties
  • Cancer Diagnosis – Methods
  • Cancer Treatment – Methods
ispartof: Contrast Media & Molecular Imaging, 2017, Vol.2017, 8 pages
description: 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. Ga is an excellent PET nuclide due to availability, nearly quantitative reaction, and short physical half-life. In this study, Ga 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. [Ga] Ga-NOTA-MAL-FSH1 can be produced within 20 min with yield and the radiochemical purity was greater than 95%. It showed that [Ga] 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 , , and % ID/g at 0.5, 1 h, and 2 h postinjection. The corresponding tumor to blood and tumor to muscle ratios were , , and and , , and , respectively. FSHR binding specificity was also demonstrated by reduced tumor uptake of [Ga] Ga-NOTA-MAL-FSH1 after coinjecting excess unlabeled FSH1 peptide. The favorable characters of [Ga] Ga-NOTA-MAL-FSH1 such as convenient synthesis and specific tumor uptake warrant its further investigation for FSHR expression imaging.
language:
source:
identifier: ISSN: 1555-4309 ; E-ISSN: 1555-4317 ; DOI: 10.1155/2017/2674502
fulltext: fulltext
issn:
  • 1555-4309
  • 15554309
  • 1555-4317
  • 15554317
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titlePET Imaging of FSHR Expression in Tumors with Ga-Labeled FSH1 Peptide
creatorPan, Donghui ; Liu, Guifeng ; Xu, Yuping ; Wang, Yanting ; Yue, Yuanyuan ; Wang, Lizhen ; Yan, Junjie ; Wang, Xinyu ; Yang, Runlin ; Yang, Min
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descriptionFSHR 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. Ga is an excellent PET nuclide due to availability, nearly quantitative reaction, and short physical half-life. In this study, Ga 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. [Ga] Ga-NOTA-MAL-FSH1 can be produced within 20 min with yield and the radiochemical purity was greater than 95%. It showed that [Ga] 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 , , and % ID/g at 0.5, 1 h, and 2 h postinjection. The corresponding tumor to blood and tumor to muscle ratios were , , and and , , and , respectively. FSHR binding specificity was also demonstrated by reduced tumor uptake of [Ga] Ga-NOTA-MAL-FSH1 after coinjecting excess unlabeled FSH1 peptide. The favorable characters of [Ga] Ga-NOTA-MAL-FSH1 such as convenient synthesis and specific tumor uptake warrant its further investigation for FSHR expression imaging.
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descriptionFSHR 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. Ga is an excellent PET nuclide due to availability, nearly quantitative reaction, and short physical half-life. In this study, Ga 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. [Ga] Ga-NOTA-MAL-FSH1 can be produced within 20 min with yield and the radiochemical purity was greater than 95%. It showed that [Ga] 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 , , and % ID/g at 0.5, 1 h, and 2 h postinjection. The corresponding tumor to blood and tumor to muscle ratios were , , and and , , and , respectively. FSHR binding specificity was also demonstrated by reduced tumor uptake of [Ga] Ga-NOTA-MAL-FSH1 after coinjecting excess unlabeled FSH1 peptide. The favorable characters of [Ga] Ga-NOTA-MAL-FSH1 such as convenient synthesis and specific tumor uptake warrant its further investigation for FSHR expression imaging.
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abstractFSHR 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. Ga is an excellent PET nuclide due to availability, nearly quantitative reaction, and short physical half-life. In this study, Ga 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. [Ga] Ga-NOTA-MAL-FSH1 can be produced within 20 min with yield and the radiochemical purity was greater than 95%. It showed that [Ga] 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 , , and % ID/g at 0.5, 1 h, and 2 h postinjection. The corresponding tumor to blood and tumor to muscle ratios were , , and and , , and , respectively. FSHR binding specificity was also demonstrated by reduced tumor uptake of [Ga] Ga-NOTA-MAL-FSH1 after coinjecting excess unlabeled FSH1 peptide. The favorable characters of [Ga] Ga-NOTA-MAL-FSH1 such as convenient synthesis and specific tumor uptake warrant its further investigation for FSHR expression imaging.
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