Figure 6. Tripeptide portion of ERG occupies a site overlapping with the allosteric modulator, LY2119620, in the muscarinic M2 receptor.
Alignment of the 5-HT2B (blue) and muscarinic M2 (green; PDB 4MQS) receptor crystal structures show that M2 orthosteric agonist iperoxo (IPX) and the ergoline nucleus of ERG occupy the same site deep in the helical bundle. Similary, the tripeptide portion of ERG and M2 allosteric modulator, LY2119620 (LY), also occupy the same site encompassing the extracellular portion of the receptor.
