Orthosteric and allosteric binding sites of
CB1R. (A) Extracellular
view of the orthosteric and allosteric sites of CB1R (PDB ID 6KQI). Important orthosteric
site residues S1732.60, V1963.32, I267ECL2, W3566.48, and S3837.39, are shown in licorice
representations (yellow). The CB1R agonist, CP55940 (purple), is shown
in the orthosteric site, while the allosteric NAM, ORG27569, is shown
in combined licorice and surface representations (light blue). (B)
Membrane view of the orthosteric and allosteric binding sites of CB1R.
Some of the key allosteric site residues, H1542.41, G1572.44, V1612.48, V2344.43, and W2414.50, are shown in the licorice representation (magenta). ORG27569
is shown in light representation (light blue), while the agonist is
shown in combined licorice and surface representations.