Facile Method for the Rapid Construction of Folate Targeted Fluorescent Agents for Imaging and Therapeutics for Cancer and Inflammatory Disease

The high affinity folate receptor (FR) is overexpressed on approximately 80% of all cancer types and activated macrophages associated with numerous inflammatory conditions. Consequently, FR has emerged as an attractive target for the selective delivery of folate guided therapeutic agents and for development of diagnostic strategies that are able to identify folate receptor positive cancer and immune cells in both in vitro and in vivo assays. This report describes a rapid method for the construction of a folate fluorophore targeting ligand with a biotin functional group, for the facile and rapid conjugation of streptavidin species containing either imaging agents for multimodal imaging or therapeutic agents. This strategy should prove useful for other targeting ligands and surface labeling schemes