X-ray screening identifies active site and allosteric inhibitors of SARS-CoV-2 main protease

S Günther, PYA Reinke, Y Fernández-García, J Lieske… - Science, 2021 - science.org
The coronavirus disease (COVID-19) caused by SARS-CoV-2 is creating tremendous
human suffering. To date, no effective drug is available to directly treat the disease. In a …

The role of NMDA receptor in neurobiology and treatment of major depressive disorder: evidence from translational research

M Amidfar, M Woelfer, GZ Reus, J Quevedo… - Progress in Neuro …, 2019 - Elsevier
There is accumulating evidence demonstrating that dysfunction of glutamatergic
neurotransmission, particularly via N-methyl-d-aspartate (NMDA) receptors, is involved in …

A structural biology perspective on NMDA receptor pharmacology and function

MC Regan, A Romero-Hernandez… - Current opinion in …, 2015 - Elsevier
Highlights•The NMDA receptor is a membrane protein critical to mammalian learning and
memory.•Heterotetrameric NMDARs consist of three structured domains that regulate ion …

Alcohol related changes in regulation of NMDA receptor functions

J Nagy - Current neuropharmacology, 2008 - ingentaconnect.com
Long-term alcohol exposure may lead to development of alcohol dependence in
consequence of altered neurotransmitter functions. Accumulating evidence suggests that the …

A novel binding mode reveals two distinct classes of NMDA receptor GluN2B-selective antagonists

D Stroebel, DL Buhl, JD Knafels, PK Chanda… - Molecular …, 2016 - ASPET
N-methyl-d-aspartate receptors (NMDARs) are glutamate-gated ion channels that play key
roles in brain physiology and pathology. Because numerous pathologic conditions involve …

Glutamate receptors and Parkinson's disease: opportunities for intervention

MJ Marino, O Valenti, PJ Conn - Drugs & aging, 2003 - Springer
Parkinson's disease is a debilitating neurodegenerative movement disorder that is the result
of a degeneration of dopaminergic neurons in the substantia nigra pars compacta. The …

Sex-related differences in NMDA-evoked rat masseter muscle afferent discharge result from estrogen-mediated modulation of peripheral NMDA receptor activity

XD Dong, MK Mann, U Kumar, P Svensson… - Neuroscience, 2007 - Elsevier
In the present study, the hypothesis that sex-related differences in glutamate-evoked rat
masseter muscle afferent discharge may result from estrogen-related modulation of …

NR2B selective NMDA antagonists: the evolution of the ifenprodil-type pharmacophore

I Borza, G Domany - Current topics in medicinal chemistry, 2006 - ingentaconnect.com
The quest for NR2B subtype selective NMDA antagonists started almost twenty years ago.
The structure of ifenprodil, the prototype of this group of compounds, inspired many …

Ifenprodil stereoisomers: synthesis, absolute configuration, and correlation with biological activity

E Bechthold, JA Schreiber, K Lehmkuhl… - Journal of Medicinal …, 2021 - ACS Publications
Ifenprodil (1) is a potent GluN2B-selective N-methyl-d-aspartate (NMDA) receptor antagonist
that is used as a cerebral vasodilator and has been examined in clinical trials for the …

Human immunodeficiency virus-1 Tat protein increases the number of inhibitory synapses between hippocampal neurons in culture

NJ Hargus, SA Thayer - Journal of Neuroscience, 2013 - Soc Neuroscience
Synaptodendritic damage correlates with cognitive decline in many neurodegenerative
diseases, including human immunodeficiency virus-1 (HIV-1)-associated neurocognitive …