5-carboxytetramethylrhodamine-succinimidyl-ester and Glioblastoma

Glioblastoma multiforme is the most common and most lethal primary brain tumor in humans, with median survival of approximately 1 year. Owing to the ability of glioma cells to aggressively infiltrate normal brain tissue and survive exposure to current adjuvant therapies, there is a great need for specific targeted nanoplatforms capable of delivering both therapeutic and imaging agents directly to invasive tumor cells.. Gadolinium-containing endohedral fullerenes, highly efficient contrast agents for MRI, were functionalized and conjugated with a tumor-specific peptide and assessed for their ability to bind to glioma cells in vitro.. We report the successful conjugation of the carboxyl functionalized metallofullerene Gd(3)N@C(80)(OH)(-26)(CH(2)CH(2)COOH)(-16) to IL-13 peptides and the successful targeting ability towards brain tumor cells that overexpress the IL-13 receptor (IL-13Rα2).. These studies demonstrate that IL-13 peptide-conjugated gadolinium metallofullerenes could serve as a platform to deliver imaging and therapeutic agents to tumor cells.

Topics: Amino Acid Sequence; Animals; Brain Neoplasms; Contrast Media; Coordination Complexes; Drug Delivery Systems; Fullerenes; Glioblastoma; Humans; Interleukin-13; Magnetic Resonance Imaging; Mice; Mice, Nude; Molecular Sequence Data; Nanoshells; Peptides; Receptors, Interleukin-13; Rhodamines