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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 Schirrmacher, Ralf ; Ralf Schirrmacher

Contrast media and molecular imaging, 2017-01, Vol.2017, p.6873684-10 [Periódico revisado por pares]

England: Hindawi

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Título:
High Contrast PET Imaging of GRPR Expression in Prostate Cancer Using Cobalt-Labeled Bombesin Antagonist RM26
Autor: Mitran, Bogdan ; Thisgaard, Helge ; Rosenström, Ulrika ; Dam, Johan Hygum ; Larhed, Mats ; Tolmachev, Vladimir ; Orlova, Anna
Schirrmacher, Ralf ; Ralf Schirrmacher
Assuntos: Affinity ; Allografts ; Binding ; Biological effects ; Biology ; Blood ; Bombesin ; Breast cancer ; Cancer ; Cobalt ; Computed tomography ; Feasibility studies ; Gastrin ; Image contrast ; In-Vivo Evaluation ; Kidneys ; Labeling ; Medical imaging ; Microwaves ; Nuclear medicine ; Organs ; Peptides ; Positron emission ; Positron-Emission-Tomography ; Prostate ; Prostate cancer ; Proteins ; Radioactivity ; Radiolabeled Peptides ; Reabsorption ; Receptor-Positive Tumors ; Single photon emission computed tomography ; Stability ; Therapy ; Tomography ; Tumors ; Visualization ; Xenografts ; Xenotransplantation
É parte de: Contrast media and molecular imaging, 2017-01, Vol.2017, p.6873684-10
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Academic Editor: Ralf Schirrmacher
Descrição: 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 a 55Co-labeled PET agent based on GRPR antagonist RM26 for visualization of GRPR-expressing tumors. Labeling with 57Co and 55Co, stability, binding specificity, and in vitro and in vivo characteristics of 57Co-NOTA-PEG2-RM26 were studied. NOTA-PEG2-RM26 was successfully radiolabeled with 57Co and 55Co 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-to-blood 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 (using 55Co) and SPECT/CT (using 57Co) images of PC-3 xenografts. The initial biological results suggest that 55Co-NOTA-PEG2-RM26 is a promising tracer for PET visualization of GRPR-expressing tumors.
Editor: England: Hindawi
Idioma: Inglês

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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 Schirrmacher, Ralf ; Ralf Schirrmacher

England: Hindawi

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