EXPERIMENTAL MODELS FOR THE IDENTIFICATION OF NEW RADIOLABELED COMPOUNDS NEEDED FOR THE DIAGNOSIS AND INTERNAL RADIO-THERAPY OF MALIGNANT MELANOMA

Authors: Maria Alexandra BUDIRINCĂ, Maria Iuliana GRUIA, Marieta PANAIT, Valentina NEGOIȚĂ, Rodica ANGHEL

Abstract:

In oncology, positron emission tomography (PET) uses diagnostic / therapeutic agents based on radiolabeled peptides, which bind selectively and specifically to receptors overexpressed on the surface of malignant tumor cells. For some tumors (hepatocellular carcinomas, sarcomas), PET / (FDG) use should be cautious, due to the low rate of glucose metabolism, low levels of Glut-1 transporters, or high glucose-6-phosphatase activity. Studies in the field have led to the development of an impressive number of usable tracers. Research is focused on obtaining new radiopharmaceuticals designed to improve the boundaries between tumor and normal tissues. One of the major objectives is to obtain radionuclides with adequate nuclear properties, able to incorporate into the tumor mass in order to destroy malignant transformed cells, and to assess the specific biological activity of radiolabeled biomolecules. The purpose of this study was to create an experimental model for investigating the potential biological effects of 68Ga-labeled peptides on melanoma target cells. To this end, two new compounds, 68Ga-DOTA-c(RGDfk) and68Ga-NODAGA-c (RGDfk) were investigated, as well as their biological effects, by apoptosis and cell cycle analysis. This type of study demonstrates the ability of 68Ga-labeled peptides to exert significant inhibitory effects on murine tumor cells.

Keywords:
  • experimental model
  • malignant melanoma
  • radiolabeled therapeutic agents