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AbstractAbstract
[en] Early diagnosis and treatment of melanoma, a cutaneous tumor with a serious prognosis, is extremely important for optimal clinical outcome. Phage display peptide libraries are a useful screening resource for identifying bioactive peptides that interact with cancer targets. The aim of this study was the evaluation of two technetium-99m tracers for angio genesis detection in melanoma model, using cyclic peguilated pentapeptide with RGD and NGR motifs conjugated with bifunctional chelator MAG3. The conjugated peptides (10 μL of a μg/μL solution) were labeled with technetium-99m using a sodium tartrate buffer. Radiochemical evaluation was done by ITLC and confirmed by HPLC. Partition coefficient was determined and internalization assays were performed in two melanoma cells (B16F10 and SKMEL28). Biodistribution evaluation of the tracers was done in healthy animals at different times and also in mice bearing the tumor cells at 120 min post injection. Blocking studies were also conducted by co-injection of cold peptides. The conjugated showed the same profile in many evaluations. They were radiolabeled with high radiochemical purity (>97%). Both were hydrophilic, with preferential renal excretion. Tumor uptake was higher for human melanoma cells than for murinic melanoma cells, specially for 99mTc-MAG3-PEG8-c(RGDyK) (7.85±±2.34 %ID/g) at 120 min post injection. The performance of 99mTc-MAG3-PEG8-c(RGDyk) was much better than NGR tracer concerning human melanoma uptake and might be considered in future investigations focusing radiotracers for melanoma diagnosis. (author)
Original Title
Estudo comparativo de radiofarmacos para angiogenese na deteccao de melanoma
Primary Subject
Source
2011; 86 p; Diss. (M.Sc.)
Record Type
Miscellaneous
Literature Type
Thesis/Dissertation
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Country of publication
ANIMALS, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, CARCINOMAS, CHROMATOGRAPHY, DISEASES, DRUGS, EPITHELIOMAS, EVALUATION, HOURS LIVING RADIOISOTOPES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LABELLED COMPOUNDS, LIQUID COLUMN CHROMATOGRAPHY, MAMMALS, MATERIALS, MICE, NEOPLASMS, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, PEPTIDES, PROTEINS, RADIOACTIVE MATERIALS, RADIOISOTOPES, RODENTS, SEPARATION PROCESSES, TECHNETIUM ISOTOPES, TRANSGENIC ANIMALS, VERTEBRATES, YEARS LIVING RADIOISOTOPES
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