Extended Data Fig. 6: GluA2-γ2IS-1 map examples and workflow for elucidating GYKI-52466 binding pocket. | Nature Structural & Molecular Biology

Extended Data Fig. 6: GluA2-γ2IS-1 map examples and workflow for elucidating GYKI-52466 binding pocket.

From: Allosteric competition and inhibition in AMPA receptors

Extended Data Fig. 6

(a) Examples of Cryo-EM map for the AMPAR TMD and Glu-bound LBD. (b) Symmetry expansion was applied through to the isolated GluA2-γ2IS-1 TMD to increase the effective particle count of the GYKI-52466 binding pocket. (c) Following expansion one of the four GYKI-52466 binding pockets was masked and then the mask inverted to subtract away the remaining TMD structure. (d) Local refinement of the isolated GYKI-52466 binding pocket resolved the pocket to 2.21 Å resolution. (e) Cryo-EM map of the GYKI-52466 pocket shown from left to right at thresholds of 0.8, 0.6, and 0.4. (f) Comparisons between PPLM binding pockets and GYKI-52466 from this study.

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