Shining bright: Fluorescent tools for drug discovery, development and delivery (PDF)

In chemical biology, the fluorescent labeling of molecules and usage of fluorescence-based imaging techniques for visualizing molecular interactions at a subcellular level is a key feature and contributes significantly to the elucidation of disease mechanisms. Furthermore, potential drug target sites can be identified, drugs acting on such sites can be developed, and by their labeling, the interactions of drugs and targets can be uncovered. In this work, innovative approaches for the fluorescent labeling of proteins, nucleic acids, and drugs are presented. A novel methodology for the facile synthesis of a versatile, functionalized, water-soluble, and tunable fluorescent probe has been developed. As a class of promising drug candidates, oligonucleotides were labeled in a dual-color readout DNA/RNA “Traffic Lights” concept that allows reliable tracking of cellular delivery, target binding, and structural integrity of nucleic acids. To ensure efficient early detection of diseases, a melanocyte-specific compound has been synthesized with the goal of enabling melanoma detection via non-invasive fluorescence microscopy. Once a cancerous disease with a solid tumor is detected, the efficient transport of a drug to the tumor site and local accumulation is of meaningful impact. A polymeric nanocarrier system for targeted tumor transport and triggered drug release has been developed.