Comparative evaluation of linear and cyclic 99mTc-RGD peptides for targeting of integrins in tumor angiogenesis

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Comparative evaluation of linear and cyclic 99mTc-RGD peptides for targeting of integrins in tumor angiogenesis (EN)

Psimadas, D (EN)
Zikos, C (EN)
Xanthopoulos, S (EN)
Bouziotis, P (EN)
Fani, M (EN)
Loudos, GK (EN)
Varvarigou, AD (EN)

journalArticle (EN)

2014-03-01T01:23:42Z
2006 (EN)


Cell adhesion molecules, such as integrins, play a vital role in angiogenesis, a key pathway for tumor growth, invasion and metastasis. The integrin a(v)beta(3), which recognizes the RGD sequence (Arg-Gly-Asp), may provide a target for in vivo tumor imaging. A linear and a cyclic RGD peptide derivative (RGDfK-His and cRGDfK-His, respectively), labelled via the precursor [Tc-99m(H2O)(3)(CO)(3)](+), were comparatively evaluated and their radiobiological properties were assessed in normal and tumor-bearing mice. Biodistribution studies showed non-specific uptake in all organs, rapid blood clearance and elimination via the hepatobiliary and urinary systems. Tumor uptake was higher for the cyclic radiolabelled derivative, as the both biodistribution and imaging studies suggested. The cRGDfK-His, labelled via the fac-[Tc-99m(CO)(3)]-core, may prove to be a useful tool for early tumor detection. (EN)

Oncology (EN)

Humans (EN)
Technetium (EN)
Breast Neoplasms (EN)
Tissue Distribution (EN)
Angiogenesis (EN)
mouse (EN)
drug excretion (EN)
arginylglycylaspartic acid tc 99m (EN)
protein targeting (EN)
drug uptake (EN)
animal model (EN)
female (EN)
Radiopharmaceuticals (EN)
tumor vascularization (EN)
radiobiology (EN)
angiogenesis (EN)
cancer diagnosis (EN)
human cell (EN)
RGD (EN)
animal experiment (EN)
article (EN)
Peptides, Cyclic (EN)
vitronectin receptor (EN)
Mice, Nude (EN)
animal tissue (EN)
Cell Line, Tumor (EN)
nonhuman (EN)
Mice (EN)
Integrins (EN)
drug clearance (EN)
technetium 99m (EN)
unclassified drug (EN)
Oligopeptides (EN)
tumor xenograft (EN)
Neovascularization, Pathologic (EN)
Integrin alphaVbeta3 (EN)
drug liver level (EN)
amino acid sequence (EN)
metastasis (EN)
tumor growth (EN)
Female (EN)
priority journal (EN)
integrin (EN)
Technetium Compounds (EN)
human (EN)
Carbonyls (EN)
drug urine level (EN)
drug targeting (EN)
Animals (EN)
cancer invasion (EN)
controlled study (EN)
drug distribution (EN)
arginylglycylaspartic acid (EN)

Anticancer Research (EN)

English

INT INST ANTICANCER RESEARCH (EN)




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