High contrast pet imaging of GRPR expression in prostate cancer using cobalt-labeled bombesin antagonist RM26

Bogdan Mitran, Helge Thisgaard, Ulrika Rosenström, Johan Hygum Dam, Mats Larhed, Vladimir Tolmachev, Anna Orlova*

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Resumé

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.

OriginalsprogEngelsk
Artikelnummer6873684
TidsskriftContrast Media & Molecular Imaging (Print)
Vol/bind2017
Antal sider10
ISSN1555-4309
DOI
StatusUdgivet - 2017

Fingeraftryk

Bombesin Receptors
Cobalt
Prostatic Neoplasms
Radioactivity
Neoplasms
Peptide Receptors
Heterografts
1,4,7-triazacyclononane-N,N',N''-triacetic acid
Kidney
Liver

Citer dette

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title = "High contrast pet imaging of GRPR expression in prostate cancer using cobalt-labeled bombesin antagonist RM26",
abstract = "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.",
author = "Bogdan Mitran and Helge Thisgaard and Ulrika Rosenstr{\"o}m and Dam, {Johan Hygum} and Mats Larhed and Vladimir Tolmachev and Anna Orlova",
year = "2017",
doi = "10.1155/2017/6873684",
language = "English",
volume = "2017",
journal = "Contrast Media & Molecular Imaging (Print)",
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High contrast pet imaging of GRPR expression in prostate cancer using cobalt-labeled bombesin antagonist RM26. / Mitran, Bogdan; Thisgaard, Helge; Rosenström, Ulrika; Dam, Johan Hygum; Larhed, Mats; Tolmachev, Vladimir; Orlova, Anna.

I: Contrast Media & Molecular Imaging (Print), Bind 2017, 6873684, 2017.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

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

PY - 2017

Y1 - 2017

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.

U2 - 10.1155/2017/6873684

DO - 10.1155/2017/6873684

M3 - Journal article

VL - 2017

JO - Contrast Media & Molecular Imaging (Print)

JF - Contrast Media & Molecular Imaging (Print)

SN - 1555-4309

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