TSPO targeted dendrimer imaging agent: synthesis, characterization, and cellular internalization.

Abstract

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 of high-affinity conjugable ligands. The 18 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.

• Authors: Lynn E Samuelson, Madeline J Dukes, Colette R Hunt, Jonathan D Casey, Darryl J Bornhop
• Journal: Bioconjugate chemistry (Bioconjug Chem) Vol. 20 Issue 11 Pg. 2082-9 (Nov 2009) ISSN: 1520-4812 [Electronic] United States
• PMID: 19863077 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, U.S. Gov't, Non-P.H.S.)

Chemical References

• Dendrimers
• Drug Carriers
• Mitochondrial Proteins
• Receptors, GABA
• TSPO protein, human

Topics

• Animals
• Cell Membrane Permeability
• Dendrimers (pharmacokinetics, therapeutic use)
• Diagnostic Imaging (methods)
• Drug Carriers (chemistry)
• Drug Delivery Systems (methods)
• Glioma (diagnosis, pathology)
• Mitochondria (metabolism)
• Mitochondrial Proteins (metabolism)
• Rats
• Receptors, GABA (analysis, metabolism)