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[99mtc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging

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National Technical University of Athens   

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[99mtc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging (EN)
Nock, B (EN)
Reubi, JC (EN)
Nikolopoulou, A (EN)
Chiotellis, E (EN)
Maina, T (EN)
Maintas, D (EN)
Loudos, G (EN)
journalArticle (EN)
2014-03-01T01:18:29Z
2003 (EN)
Demobesin 1 is a potent new GRP-R-selective bombesin (BN) analogue containing an open chain tetraamine chelator for stable technetium-99m binding. Following a convenient labelling protocol, the radiopeptide, [Tc-99m]Demobesin 1, formed in nearly quantitative yields and with high specific activities. Both unlabelled and labelled peptide demonstrated high-affinity binding in membrane preparations of the human androgen-independent prostate adenocarcinoma PC-3 cell line. The IC50 values determined for Demobesin 1 and [Tyro]BN were 0.70+/-0.08 nM and 1.5+/-0.20 nM, respectively, while the K-d defined for [Tc-99m/Tc-99g]Demobesin 1 was 0.67+/-0.10 nM. [Tc-99m]Demobesin 1 was rather stable in murine plasma, whereas it degraded rapidly in kidney and liver homogenates. After injection in healthy Swiss albino mice, [Tc-99m]Demobesin 1 accumulated very efficiently in the target organs (pancreas, intestinal tract) via a GRP-R-mediated process, as shown by in vivo receptor blocking experiments. An equally high and GRP-R-mediated uptake was exhibited by [Tc-99m]Demobesin 1 after injection in PC-3 tumour-bearing athymic mice. The initial high radioligand uptake of 16.2+/-3.1%ID/g in the PC-3 xenografts at 1 h p.i. remained at a similar level (15.61+/-1.19%ID/g) at 4 h p.i. Even after 24 h p.i., when the radioactivity had cleared from all other tissues, a value of 5.24+/-0.67%ID/g was still observed in the tumour. The high and prolonged localization of [Tc-99m]Demobesin 1 at the tumour site and its rapid background clearance are very promising qualities for GRP-R-targeted tumour imaging in man. (EN)
Radiology, Nuclear Medicine & Medical Imaging (EN)
Tumour imaging (EN)
drug degradation (EN)
drug potency (EN)
kidney metabolism (EN)
Humans (EN)
Liver (EN)
Male (EN)
Metabolic Clearance Rate (EN)
tissue distribution (EN)
evaluation (EN)
Tissue Distribution (EN)
mouse (EN)
kidney (EN)
G protein coupled receptor (EN)
Tetraamine chelator (EN)
drug uptake (EN)
gastrin releasing peptide (EN)
animal model (EN)
cancer cell culture (EN)
female (EN)
skeletal muscle (EN)
Radiopharmaceuticals (EN)
Organotechnetium Compounds (EN)
99mTc (EN)
Gastrin-Releasing Peptide (EN)
liver (EN)
liver homogenate (EN)
human cell (EN)
radiopharmaceutical agent (EN)
animal experiment (EN)
article (EN)
prostate adenocarcinoma (EN)
tumor scintiscanning (EN)
cell culture (EN)
technetium 99m demobesin 1 (EN)
prostate tumor (EN)
animal (EN)
nonhuman (EN)
metabolism (EN)
target organ (EN)
isotope labeling (EN)
drug tissue level (EN)
male (EN)
drug derivative (EN)
drug clearance (EN)
drug stability (EN)
binding affinity (EN)
unclassified drug (EN)
Cell Membrane (EN)
Neoplasm Transplantation (EN)
comparative study (EN)
pathology (EN)
tumor xenograft (EN)
cell membrane (EN)
Kidney (EN)
drug accumulation (EN)
Prostatic Neoplasms (EN)
antibody specificity (EN)
drug receptor binding (EN)
Isotope Labeling (EN)
Female (EN)
demobensin 1 technetium tc 99m (EN)
Tumor Cells, Cultured (EN)
technetium complex (EN)
cancer transplantation (EN)
human (EN)
bombesin derivative (EN)
synthesis (EN)
metabolic clearance rate (EN)
Bombesin (EN)
scintiscanning (EN)
protein binding (EN)
Organ Specificity (EN)
blood (EN)
bombesin (EN)
Gastrin releasing peptide (EN)
diagnostic agent (EN)
Animals (EN)
controlled study (EN)
drug distribution (EN)
Protein Binding (EN)
gastrin releasing peptide receptor (EN)
Muscle, Skeletal (EN)
injection (EN)
methodology (EN)
European Journal of Nuclear Medicine and Molecular Imaging (EN)
English
SPRINGER-VERLAG (EN)
National Technical University of Athens
Digital Library of National Technical University of Athens | Dspace@NTUA
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