Fig. 4: The unconventional activation mechanism of compound-110. | Nature Communications

Fig. 4: The unconventional activation mechanism of compound-110.

From: The unconventional activation of the muscarinic acetylcholine receptor M4R by diverse ligands

Fig. 4: The unconventional activation mechanism of compound-110.The alternative text for this image may have been generated using AI.

a Schematic summarizing the key translational and rotational movements contributing to M4R activation induced by compound-110. b Extracellular conformational changes from inactive (blue) to compound-110-bound active (green) M4R. c A specific ‘triangle frame’ formed by the side chains of residues Asp1123.32, Ser852.57, and Tyr4437.43 in the M4R–c110–Gi structure. d Conformational changes of residues Tyr4166.51and Trp4136.48 during M4R activation by compound-110. e Conformational changes of the NPxxY motif between inactive and compound-110-bound active M4R structures.

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