[DOT 2018] Multiple Pathway Activation in a Human M4 Muscarinic Receptor Cell-Based Assay

[DOT 2018] Multiple Pathway Activation in a
Human M4 Muscarinic Receptor Cell-Based Assay
File Name/Number:
DOT 2018

Year:
2018

In recent years it has become increasingly clear that many G protein-coupled receptors (GPCR) not only activate one single, but several different types of G proteins1. Moreover, biased ligands exist which exert differential effects on the different signaling pathways of a given GPCR. Such biased ligands may enable the development of new drugs with improved efficacy and safety. For in vitro pharmacological testing of compounds, however, the multiple coupling of a given GPCR to several different signaling pathways represents important challenges: Several pathways (instead of only one) should be measured in parallel; these different pathways may interfere with each other; and the relative contribution of the different pathways may depend on the experimental system (cell line) used. In this poster, we present a case study on the M4muscarinic acetylcholine receptor.