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. 2023 Oct 30;30(12):1936–1946. doi: 10.1038/s41594-023-01133-1

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Extended Data Fig. 5 — a, Overlays of the α1β3γ2 receptor at the α1-γ2 binding pocket for apo (dark grey) versus diazepam-bound (DZP; α1 principal face in pink and γ2 complementary face in pale yellow), showing that the pocket is highly similar. b, Equivalent view, but overlay of α1γ2-apo (dark grey) versus α5V3-apo (light grey), showing that pocket is also highly similar. The relative upward position of α5V3-apo Y49 versus α1γ2-apo Y58 is indicated (blue arrow). c, Overlay of α1γ2-DZP (pink/pale yellow) versus α5V3-apo (light grey), with the relative upward position of α5V3-apo Y49 versus α1γ2-DZP Y58 indicated (blue arrow). d, Overlay of α5V3-DZP (red/yellow) versus α5V3-apo (light grey), showing that the pocket is highly similar but binding of diazepam has caused displacement of Y49 by 2.3 Å (blue arrow). e, Overlay of α1γ2-DZP (pink/pale yellow) versus α5V3-DZP (red/yellow), showing that the downward displacement by DZP on Y49 means it now matches the position of Y58 in the α1-γ2-DZP pocket. f, Cryo-EM map of α5V3-DMCM showing the fit of the DMCM molecule into the density. The isosurface level of the protein and ligand are the same. Shown from two viewing angles. g, Structural model overlay of α5V3-apo (grey) versus α5V3-DMCM showing that Y49 does not need to move to accommodate DMCM binding. Note: The structural model of the α1-γ2-apo pocket is from the α1β3γ2 receptor bound by antagonist bicuculline, PDB 6HUK; α1γ2-DZP is from α1β3γ2 receptor bound by GABA and diazepam, PDB 6HUP. For reference, equivalent complementary face residue numbering of α5V3 Y49, A70, T133, in wild type γ2 is Y58, A79, T142 respectively.