Development of novel fluorescent probes

The development of new drug candidates drug discovery programs require versatile, sensitive pharmacological tools for ligand binding and compound screening. The incorporation of a fluorophore into chemical molecules of interest, makes fluorescent probes suitable tools for a range of applications. Fluorescent probes have been established as valuable tools in drug discovery, for instance for studying protein targets and the identification of novel hits from screening libraries. However, a major limitation of current probes is the level of chemical modification required to induce fluorescence. The incorporation of fluorophores generally results in a substantial change in chemical structure, molecular size and physiochemical properties in comparison to the parent compound. This is particularly profound for small non-peptide based hits, including those designed to pass the blood–brain barrier. As a result, they may not able to interact with the target or are poorly representative of how the parent compound interacts with the target, and additionally are often less active and drug-like. Therefore, this project focuses on the development of small drug-like fluorescent fluorophores, which will allow for more accurate modelling of the mechanism of action of the parent compound, and opening up the possibility of using such probes for in vivo applications.