A research team from Würzburg, Bonn and Milan has now discovered a completely novel approach: They identified an area in the protein structure of a GPCR that can be used as a "switch point" for signals.
What the scientists achieved: With specially designed agents, they were able to activate a certain GPCR, the so-called muscarinic receptor, at a particular point while giving the response signal a specific direction at another point. In this way, the activation does not set off several signals, but only one – the desired one in each case. "Numerous members of the GPCR family have such switch points in their protein structure, so that further receptors might be regulated in this novel way," says Holzgrabe. This opens the prospect of developing innovative drugs which manipulate the cell function in a more targeted way, enabling a more effective and well tolerated treatment. Next, the researchers are going to design further agents in order to get more insights into the signal transduction of GPC receptors. (© University of Würzburg / AcademiaNet)