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. 2021 Dec 6;10:e70188. doi: 10.7554/eLife.70188

Figure 1. Allosteric binding sites in the different classes of G protein-coupled receptors (GPCRs).

Figure 1.

(A, B) Scheme and structure of the transmembrane domain (TMD) representative of the diversity of the binding sites for allosteric modulators (filled blue circles or blue spheres) in selected human class A and B GPCRs (muscarinic M2 receptor PDB 4MQT [1], purinergic P2Y1 receptor PDB 4XNV [2], corticotropin-releasing factor receptor 1 PDB 4K5Y [3], and β2 adrenergic receptor PDB 5X7D [4]) (A), as well as in the class C homodimer mGluR5 (PDB 6N51) bound to a NAM (PDB 4OO9) and the heterodimer GABABR bound to GS39783 (PDB 6UO8) (B). In classes A and B, the allosteric modulators were shown to bind to different sites within and outside of the TM bundle, in contrast to the orthosteric ligand (black triangle).