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AbstractAbstract
[en] Integrin αvβ3 has a critical role in tumor angio genesis and metastasis. Radiolabelled peptides based on the Arg-Gly-Asp (RGD) sequence have been reported as radiopharmaceuticals with high affinity and selectivity for the αvβ3 integrin. The aim of this study was to label c-DOTA-RGD and c-DOTA-RGDf peptides with 177Lu and to evaluate their in vitro and in vivo stability as potential specific therapeutic radiopharmaceuticals. Labelled was carried out by direct reaction of 177LuCl3 with c-DOTA-RGD peptides in 1 M acetate buffer ph 5.5 at 90o C for 30 min. Radiochemical purity and stability studies were realized by reversed phase HPLC and I TLC-Sg analyses in human serum and saline solution. Biological recognition was performed using MCF7 tumor cells (positive αvβ3) and in athymic mice with induced MCF7 tumors. Molecular mechanics and quantum mechanics calculations were performed to explain experimental results associated with the molecular recognition. 177Lu-DOTA-RGD and 177Lu-DOTA-RGDf were obtained with radiochemical purities > 95%, showing adequate in vitro and in vivo stability and specific binding to □v□3 receptors. (Author)
Original Title
Radiomarcado del peptido c-DOTA-RGD y c-DOTA-RGDf con 177Lu y evaluacion de su estabilidad in vitro e in vivo
Primary Subject
Source
2010; 101 p; Thesis (Pharmacist)
Record Type
Miscellaneous
Literature Type
Thesis/Dissertation
Report Number
Country of publication
ANIMAL CELLS, ANIMALS, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, CARBOXYLIC ACID SALTS, CHEMISTRY, DAYS LIVING RADIOISOTOPES, DISEASES, DISPERSIONS, DRUGS, HOMOGENEOUS MIXTURES, INTERMEDIATE MASS NUCLEI, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LABELLED COMPOUNDS, LUTETIUM ISOTOPES, MAMMALS, MATERIALS, MECHANICS, MEMBRANE PROTEINS, MIXTURES, NUCLEAR REACTIONS, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, PROTEINS, RADIOACTIVE MATERIALS, RADIOISOTOPES, RARE EARTH NUCLEI, RODENTS, VERTEBRATES
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