TY - JOUR
T1 - High contrast pet imaging of GRPR expression in prostate cancer using cobalt-labeled bombesin antagonist RM26
AU - Mitran, Bogdan
AU - Thisgaard, Helge
AU - Rosenström, Ulrika
AU - Dam, Johan Hygum
AU - Larhed, Mats
AU - Tolmachev, Vladimir
AU - Orlova, Anna
N1 - Funding Information:
The molecular imaging work in this publication has been supported by the Wallenberg infrastructure for PET-MRI (WIPPET) at SciLifeLab Pilot Facility for Preclinical PET-MRI, a Swedish nationally available imaging platform at Uppsala University, Sweden, financed by Knut and Alice Wallenberg Foundation (SPECT/CT). This work was supported by the Swedish Cancer Society (Grants CAN2014/474 (Anna Orlova) and CAN2015/350 (Vladimir Tolmachev)) andtheSwedishResearchCouncil(Grants2015-02509(Anna Orlova) and 2015-02353 (Vladimir Tolmachev)), which are acknowledged for financial support. The authors acknowledge the Danish Molecular Biomedical Imaging Center (DaMBIC, University of Southern Denmark) for the use of the bioimaging facilities and they thank Christina Baun, Department of Nuclear Medicine, Odense University Hospital, for her technical assistance.
Publisher Copyright:
© 2017 Bogdan Mitran et al.
Copyright:
Copyright 2018 Elsevier B.V., All rights reserved.
PY - 2017/8/10
Y1 - 2017/8/10
N2 - High gastrin releasing peptide receptor (GRPR) expression is associated with numerous cancers including prostate and breast cancer.The aim of the current study was to develop a55Co-labeled PET agent based on GRPR antagonist RM26 for visualization of GRPR-expressing tumors. Labeling with57Co and55Co, stability, binding specificity, and in vitro and in vivo characteristics of57Co-NOTA-PEG2-RM26 were studied.NOTA-PEG2-RM26 was successfully radiolabeled with57Co and55Co with high yields and demonstrated high stability.The radiopeptide showed retained binding specificity to GRPR in vitro and in vivo.57Co-NOTA-PEG2- RM26 biodistribution in mice was characterized by rapid clearance of radioactivity from blood and normal non-GRPR-expressing organs and low hepatic uptake.The clearance was predominantly renal with a low degree of radioactivity reabsorption. Tumor-toblood ratios were approximately 200 (3 h pi) and 1000 (24 h pi).The favorable biodistribution of cobalt-labeled NOTA-PEG2-RM26 translated into high contrast preclinical PET/CT (using55Co) and SPECT/CT (using57Co) images of PC-3 xenografts.The initial biological results suggest that55Co-NOTA-PEG2-RM26 is a promising tracer for PET visualization of GRPR-expressing tumors.
AB - High gastrin releasing peptide receptor (GRPR) expression is associated with numerous cancers including prostate and breast cancer.The aim of the current study was to develop a55Co-labeled PET agent based on GRPR antagonist RM26 for visualization of GRPR-expressing tumors. Labeling with57Co and55Co, stability, binding specificity, and in vitro and in vivo characteristics of57Co-NOTA-PEG2-RM26 were studied.NOTA-PEG2-RM26 was successfully radiolabeled with57Co and55Co with high yields and demonstrated high stability.The radiopeptide showed retained binding specificity to GRPR in vitro and in vivo.57Co-NOTA-PEG2- RM26 biodistribution in mice was characterized by rapid clearance of radioactivity from blood and normal non-GRPR-expressing organs and low hepatic uptake.The clearance was predominantly renal with a low degree of radioactivity reabsorption. Tumor-toblood ratios were approximately 200 (3 h pi) and 1000 (24 h pi).The favorable biodistribution of cobalt-labeled NOTA-PEG2-RM26 translated into high contrast preclinical PET/CT (using55Co) and SPECT/CT (using57Co) images of PC-3 xenografts.The initial biological results suggest that55Co-NOTA-PEG2-RM26 is a promising tracer for PET visualization of GRPR-expressing tumors.
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U2 - 10.1155/2017/6873684
DO - 10.1155/2017/6873684
M3 - Article
C2 - 29097932
AN - SCOPUS:85028513790
VL - 2017
JO - Contrast Media and Molecular Imaging
JF - Contrast Media and Molecular Imaging
SN - 1555-4309
M1 - 6873684
ER -