Structure, function, and pharmacology of glutamate receptor ion channels

KB Hansen, LP Wollmuth, D Bowie, H Furukawa… - Pharmacological …, 2021 - ASPET
Many physiologic effects of l-glutamate, the major excitatory neurotransmitter in the
mammalian central nervous system, are mediated via signaling by ionotropic glutamate …

Positive allosteric modulation of NMDA receptors: mechanisms, physiological impact and therapeutic potential

C Geoffroy, P Paoletti, L Mony - The Journal of Physiology, 2022 - Wiley Online Library
NMDA receptors (NMDARs) are glutamate‐gated ion channels that play key roles in
synaptic transmission and plasticity. Both hyper‐and hypo‐activation of NMDARs are …

Positive and Negative Allosteric Modulators of N-Methyl-d-aspartate (NMDA) Receptors: Structure–Activity Relationships and Mechanisms of Action

ES Burnell, M Irvine, G Fang, K Sapkota… - Journal of medicinal …, 2018 - ACS Publications
Excitatory activity in the CNS is predominately mediated by l-glutamate through several
families of l-glutamate neurotransmitter receptors. Of these, the N-methyl-d-aspartate …

[HTML][HTML] Differential regulation of STP, LTP and LTD by structurally diverse NMDA receptor subunit-specific positive allosteric modulators

G France, R Volianskis, R Ingram, N Bannister… - …, 2022 - Elsevier
Different types of memory are thought to rely on different types of synaptic plasticity, many of
which depend on the activation of the N-Methyl-D Aspartate (NMDA) subtype of glutamate …

Biased modulators of NMDA receptors control channel opening and ion selectivity

RE Perszyk, SA Swanger, C Shelley, A Khatri… - Nature chemical …, 2020 - nature.com
Allosteric modulators of ion channels typically alter the transitions rates between
conformational states without changing the properties of the open pore. Here we describe a …

Drug development in channelopathies: Allosteric modulation of ligand-gated and voltage-gated ion channels

Y Zhang, K Wang, Z Yu - Journal of medicinal chemistry, 2020 - ACS Publications
Ion channels have been characterized as promising drug targets for treatment of numerous
human diseases. Functions of ion channels can be fine-tuned by allosteric modulators …

Higher ambient synaptic glutamate at inhibitory versus excitatory neurons differentially impacts NMDA receptor activity

L Yao, T Grand, JE Hanson, P Paoletti… - Nature …, 2018 - nature.com
Selective disruption of synaptic drive to inhibitory neurons could contribute to the
pathophysiology of various brain disorders. We have previously identified a GluN2A …

Discovery of Novel and Potent N-Methyl-d-aspartate Receptor Positive Allosteric Modulators with Antidepressant-like Activity in Rodent Models

Z Li, G Cai, F Fang, W Li, M Fan, J Lian… - Journal of Medicinal …, 2021 - ACS Publications
N-Methyl-d-aspartate receptors (NMDARs) are glutamate-gated Na+ and Ca2+-permeable
ion channels involved in excitatory synaptic transmission and synaptic plasticity. NMDAR …

Protein quality control of N-methyl-D-aspartate receptors

TM Benske, TW Mu, YJ Wang - Frontiers in cellular neuroscience, 2022 - frontiersin.org
N-methyl-d-aspartate receptors (NMDARs) are glutamate-gated cation channels that
mediate excitatory neurotransmission and are critical for synaptic development and plasticity …

The NMDA receptor intracellular C-terminal domains reciprocally interact with allosteric modulators

K Sapkota, K Dore, K Tang, M Irvine, G Fang… - Biochemical …, 2019 - Elsevier
N-methyl-d-aspartate receptors (NMDARs) have multiple prominent roles in CNS function
but their excessive or insufficient activity contributes to neuropathological/psychiatric …