Focus on G-protein coupled receptors: Specific transport of drug through receptor internalization [Schwerpunkt G-Protein-gekoppelte Rezeptoren: Spezifischer Wirkstoff transport durch Rezeptorinternalisierung]

摘要

G-protein coupled receptors (GPCRs) are involved in many physiological and pathophysiological roles. Many important drugs act on GPCRs, either by blocking them (antagonists) or by mimicking the natural ligand (agonists). As GPCRs have been shown to internalize a new concept is currently investigated: application of agonistic ligands fused to drugs to allow selective uptake into specific cells. This has been proven for selective uptake into tumour cells but may be expanded to other systems that selectively express GPCRs.