Fig. 6: Allosteric landscape of AMPARs.
From: Allosteric competition and inhibition in AMPA receptors
a, Activation of AMPARs in the presence of the negative allosteric modulator GYKI-52466 produces the allosterically inhibited state, which we show in this study. In contrast, activation of AMPARs in the presence of the positive allosteric modulator CTZ produces the activated state. b, When both CTZ and GYKI-52466 are present, both can bind to the resting state of the receptor; however, after Glu binding, GYKI-52466 outcompetes CTZ to control the AMPAR LBD, resulting in CTZ being displaced and inhibition of the receptor.
