Entwicklung von molekularen Werkzeugen zur Untersuchung der intrazellulären allosterischen Bindungstasche von Chemokinrezeptoren

The discovery of intracellular allosteric binding sites (IABS) in GPCRs opens new avenues for drug development, particularly for receptors where traditional orthosteric inhibition proves insufficient. To overcome the limitations of conventional radioligand assays, an innovative NanoBRET platform was established using specially designed fluorescent probes that enable precise target engagement studies within living cells. By utilising structure-based design with TAMRA fluorophores and optimised linkers, this research successfully characterised novel binding assays for various chemokine receptors and demonstrated their effectiveness in a cellular environment.