5-carboxytetramethylrhodamine-succinimidyl-ester and valyl-alanyl-prolyl-glycine

We developed a Tc-99m and fluorescence-labeled peptide, Tc-99m TAMRA-GHEG-ECG-VAPG to target tumor cells and evaluated the diagnostic performance as a dual-modality imaging agent for tumor in a murine model. TAMRA-GHEG-ECG-VAPG was synthesized by using Fmoc solid-phase peptide synthesis. Radiolabeling of TAMRA-GHEG-ECG-VAPG with Tc-99m was done by using ligand exchange via tartrate. Binding affinity and in vitro cellular uptake studies were performed. Gamma camera imaging, biodistribution, and ex vivo imaging studies were performed in murine models with SW620 tumors. Tumor tissue slides were prepared and analyzed with immunohistochemistry by using confocal microscopy. After radiolabeling procedures with Tc-99m, Tc-99m TAMRA-GHEG-ECG-VAPG complexes were prepared in high yield (>96%). The K

Topics: Animals; Cell Line, Tumor; Female; Fluorescent Dyes; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Neoplasms, Experimental; Oligopeptides; Radiopharmaceuticals; Rhodamines; Technetium; Tissue Distribution