Muscarinic Acetylcholine Receptors
Muscarinic acetylcholine receptors belong to the Class A (rhodopsin-like family) of G protein-coupled receptors. The endogenous agonist acetylcholine can bind to five different subtypes of muscarinic acetylcholine receptors designated M1-M5. These five members are divided into two subtypes based on their primary coupling efficiency to G-proteins - M1, M3 and M5 receptors interact with Gq/11-proteins, while M2 and M4 interact with Gi/o-proteins. However, it is clear that muscarinic acetylcholine receptors can activate a wide range of signalling pathways (both G-protein mediated and G-protein independent). Structure of these receptors is particularly interesting due to the presence of allosteric binding sites.
Our workgroup has studied muscarinic acetylcholine receptors for a long time. For example, in his doctoral thesis professor Ago Rinken focused on how solubilisation of different muscarinic receptors can influence ligand binding. More recent research involves development of a screening system for the characterization of agonists, partial agonists and inverse agonists by reconstitution of M2 receptor with either Gi- or Go-proteins in Sf9 insect cells (Uustare et al. 2004). Currently, we are collaborating with Dr. Max Keller from the University of Regensburg to develop and characterize novel fluorescent ligands to study muscarinic M1, M2 and M4 receptors in fluorescence anisotropy based assay.
Our workgroup has studied muscarinic acetylcholine receptors for a long time. For example, in his doctoral thesis professor Ago Rinken focused on how solubilisation of different muscarinic receptors can influence ligand binding. More recent research involves development of a screening system for the characterization of agonists, partial agonists and inverse agonists by reconstitution of M2 receptor with either Gi- or Go-proteins in Sf9 insect cells (Uustare et al. 2004). Currently, we are collaborating with Dr. Max Keller from the University of Regensburg to develop and characterize novel fluorescent ligands to study muscarinic M1, M2 and M4 receptors in fluorescence anisotropy based assay.