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. 2016 Sep 21;91(6):1187-1189.
doi: 10.1016/j.neuron.2016.09.013.

Deeper Insights into the Allosteric Modulation of Ionotropic Glutamate Receptors

Michael C Regan  1 , Hiro Furukawa  2
Affiliations

Deeper Insights into the Allosteric Modulation of Ionotropic Glutamate Receptors

Michael C Regan et al. Neuron. .

Abstract

Two articles in this issue of Neuron (Yelshanskaya et al., 2016; Yi et al., 2016) explore the structural basis of allosteric inhibition in ionotropic glutamate receptors, providing key insights into how iGluRs function in the brain as well as how they might be pharmacologically modulated in neurological disorders and disease.

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Figures

Figure 1
Figure 1. Locations of allosteric binding sites in NMDAR and AMPAR
Allosteric binding sites (yellow spheres) could prove to be critical in the development of novel, highly-specific modulators of iGluRs. Yi, et al. (2016) characterized a site at the subunit interface between the LBDs of the NMDAR GluN1 and GluN2 subunits (left, grays and reds respectively). Yelshanskaya, et al. (2016) present structural data of inhibitor binding at the TMD/LBD interface of the homomeric AMPAR (right).
See this image and copyright information in PMC

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