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Fig. 2

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ZDB-IMAGE-221014-2
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Figures for Yu et al., 2021
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Fig. 2

Partial agonist complexes probed by electrophysiology and cryo-EM.

A. Representative cell-attached single-channel recordings of GlyR openings elicited by 100 mM taurine and 100 mM GABA, respectively.

B. Fractions of GlyR particles in the open, closed, desensitized and expanded-open states of the glycine, taurine and GABA complexes of the SMA-solubilized receptor, calculated by RELION and cisTEM as described in the Methods. Error bars represent SEM.

C. Whole cell, dose-response data for glycine, taurine and GABA. EC50 for glycine, taurine and GABA are 190 ± 20 ?M, 1050 ± 80 ?M and 28.4 ± 0.9 mM, respectively. Error bars represent SEM and n?6 cells for all experiments. Curves are normalized to the glycine maximum current recorded in each cell.

D-F. Distances (in angstrom) and conformation of residues ?2?P and 9?L in the taurine-bound, SMA-solubilized receptor in the open, desensitized and closed states.

G-I. Ion permeation pathway for taurine-bound states, calculated using HOLE and plotted as in Figure 1.

J-K. Pore radius as a function of distance along the pore axis for taurine-bound states (J) and GABA-bound states (K) of the SMA-solubilized receptor.

See also Figures S1, S3?S5, Tables S1?S3, S5, S7, Methods S1?S2 and Data S1.

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Reprinted from Cell, 184, Yu, J., Zhu, H., Lape, R., Greiner, T., Du, J., Lü, W., Sivilotti, L., Gouaux, E., Mechanism of gating and partial agonist action in the glycine receptor, 957-968.e21, Copyright (2021) with permission from Elsevier. Full text @ Cell