Melanoma affinity in mice and immunosuppressed sheep of [(125)I]N-(4-dipropylaminobutyl)-4-iodobenzamide, a new targeting agent
| Autor: | Janine Papon, Alain Croisy, Jean-Claude Madelmont, Jean-Luc Guerquin-Kern, Marie-France Moreau, Martine Bayle, Harvey Turner, Alison H. Rose, Laurence Morandeau, Pierre Labarre, Ting-Di Wu, Jean-Michel Chezal, Nicole Moins |
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| Rok vydání: | 2008 |
| Předmět: |
Male
Cancer Research Pathology medicine.medical_specialty Biodistribution media_common.quotation_subject Melanoma Experimental Spectrometry Mass Secondary Ion Melanin Iodine Radioisotopes chemistry.chemical_compound Mice Iodobenzamide medicine Animals Humans Radiology Nuclear Medicine and imaging Tissue Distribution Internalization media_common Melanosome Immunosuppression Therapy Melanins Sheep Melanoma medicine.disease Mice Inbred C57BL chemistry Cell culture Isotope Labeling Radionuclide therapy Benzamides Cancer research Molecular Medicine Female Radiopharmaceuticals |
| Zdroj: | Nuclear medicine and biology. 35(7) |
| ISSN: | 0969-8051 |
| Popis: | The increasing incidence of melanoma and the lack of effective therapy have prompted the development of new vectors, more specific to the pigmented tumor, for early detection and treatment. Targeted agents have to exhibit a rapid, high tumor uptake, long tumor retention and rapid clearance from nontarget organs. This joint work presents results obtained with a new melanoma targeting agent, [125I]-N-(4-dipropylaminobutyl)-4-iodobenzamide or [125I]BZ18. After labeling with a high specific activity, the biodistribution of the compound was investigated in two animal models, the mouse and the sheep. Melanotic tumor retention was observed lasting several days. We visualized the internalization of the agent inside the melanosomes by secondary ion mass spectroscopy imaging, we measured the affinity constants of [125I]BZ18 on a synthetic melanin model and we demonstrated a radiotoxic effect of this labeled agent on B16F0 melanoma cell culture due to its cellular internalization. From this work, [125I]BZ18 appeared a promising melanoma targeting agent in the nuclear medicine field. |
| Databáze: | OpenAIRE |
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