TSPO Targeted Dendrimer Imaging Agent: Synthesis Characterization and Cellular Internalization

摘要

While it has become common practice for dendrimers to deliver imaging and therapeutic agents there are few reported examples of cellular internalization of dendrimers. Moreover, targeting of dendrimers to the mitochondria in cells has not yet been reported. Previously, we have delivered small molecule imaging agents into glioma and breast cancer cells by targeting the translocator protein (TSPO; formerly known as the peripheral benzodiazepine receptor or PBR) with a family high affinity conjugable ligands. The 18 kiloDalton (kDa.) multimeric TSPO is expressed in steroid-producing cells, primarily on the outer mitochondrial membrane. This protein is a prime candidate for molecular targeting because tumors and other disease related cells contain high densities of TSPO. Here we present the synthesis, characterization and cellular internalization into C6 rat glioma cells of a TSPO targeted dendrimer imaging agent.