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Hormones and other neurotransmitters, but also drugs, act upon receptors. "Their active substances bind to the receptors and modify the three-dimensional receptor arrangement regulating the downstream signal pathways," says Hannes Schihada from the Institute for Pharmacology and Toxicology at the University of Würzburg (JMU).
A special case are G protein-coupled receptors (GPCR). "About 30 percent of all authorized drugs worldwide act upon these receptors," explains Hannes Schihada, "but their potential is not yet fully utilized." To date, it has not been possible to test the effect of millions of potential drugs on the GPCR arrangement within a very short time. "This has been a stumbling block to the discovery of novel pharmaceutical substances and the research of still unknown GPCRs," says Dr. Isabella Maiellaro, who is in charge of the project together with Professor Martin Lohse.
JMU - Team - Method - Determination - Activity
The JMU team has now developed a method that allows the determination of both activity and potency of GPCR ligands in living cells using high throughput technology. The scientists have published their results in the journal Communications Biology.
The name of the method is BRET (bioluminescence resonance energy transfer-based sensor design). "It can be used not only for GPCRs but...
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