Magnetic resonance imaging of tumor cells by targeting the amino acid transport system

• Published in: Bioorganic & medicinal chemistry letters 2006-08, Vol.16 (15), p.4111-4114
• Main Authors: Lattuada, Luciano, Demattio, Silvia, Vincenzi, Veronica, Cabella, Claudia, Visigalli, Massimo, Aime, Silvio, Crich, Simonetta Geninatti, Gianolio, Eliana
• Format: Article
• Language: English
• Subjects: Amino Acid Transport Systems - metabolism; Amino acid transporters; Animals; Biological and medical sciences; Cell Line, Tumor; Contrast media. Radiopharmaceuticals; Gadolinium; Gadolinium complexes; Glutamine uptake; Investigative techniques, diagnostic techniques (general aspects); Magnetic resonance imaging; Magnetic Resonance Imaging - methods; Medical sciences; Miscellaneous. Technology; Pharmacology. Drug treatments; Radiodiagnosis. Nmr imagery. Nmr spectrometry; Rats; Tumor cells
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2006.04.081

With the aim of discovering an early diagnosis of cancer by magnetic resonance imaging (MRI), we synthesized and studied six DTPA and DOTA-like gadolinium complexes conjugated to agmatine, arginine, and glutamine (e.g., 7a), able to target tumor cells by means of the glutamine transport system. An early diagnosis of cancer is crucial in the battle against this disease and the in vivo visualization of tumors at cellular level is still the most challenging goal. In order to target tumor cells, we took into account their increased metabolism and amino acid nutrients or pseudo-nutrients, which are actively transported through the cell membrane, have been chosen as vectors for new MRI contrast agents. For this reason new gadolinium complexes conjugated to agmatine, arginine, and glutamine have been synthesized and studied.