Organization and functions of mGlu and GABAB receptor complexes

JP Pin, B Bettler - Nature, 2016 - nature.com
The neurotransmitters glutamate and γ-aminobutyric acid (GABA) transmit synaptic signals
by activating fast-acting ligand-gated ion channels and more slowly acting G-protein …

Pharmacology of free fatty acid receptors and their allosteric modulators

M Grundmann, E Bender, J Schamberger… - International journal of …, 2021 - mdpi.com
The physiological function of free fatty acids (FFAs) has long been regarded as indirect in
terms of their activities as educts and products in metabolic pathways. The observation that …

Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin …

JA Christopher, SJ Aves, KA Bennett… - Journal of medicinal …, 2015 - ACS Publications
Fragment screening of a thermostabilized mGlu5 receptor using a high-concentration
radioligand binding assay enabled the identification of moderate affinity, high ligand …

Exploring the binding mechanism of metabotropic glutamate receptor 5 negative allosteric modulators in clinical trials by molecular dynamics simulations

T Fu, G Zheng, G Tu, F Yang, Y Chen… - ACS chemical …, 2018 - ACS Publications
Metabotropic glutamate receptor 5 (mGlu5) plays a key role in synaptic information storage
and memory, which is a well-known target for a variety of psychiatric and neurodegenerative …

Structures of G protein-coupled receptors reveal new opportunities for drug discovery

RM Cooke, AJH Brown, FH Marshall, JS Mason - Drug discovery today, 2015 - Elsevier
Highlights•X-ray structures are now available for more than 60 ligands and 20
GPCRs.•Structures reveal details of ligand biding that could not be predicted.•Structure …

Structure-based optimization strategies for G protein-coupled receptor (GPCR) allosteric modulators: a case study from analyses of new metabotropic glutamate …

JA Christopher, Z Orgován, M Congreve… - Journal of medicinal …, 2018 - ACS Publications
Two interesting new X-ray structures of negative allosteric modulator (NAM) ligands for the
mGlu5 receptor, M-MPEP (3) and fenobam (4), are reported. The new structures show how …

[HTML][HTML] Subtype-selective mechanisms of negative allosteric modulators binding to group I metabotropic glutamate receptors

T Fu, G Tu, M Ping, G Zheng, F Yang, J Yang… - Acta Pharmacologica …, 2021 - nature.com
Group I metabotropic glutamate receptors (mGlu1 and mGlu5) are promising targets for
multiple psychiatric and neurodegenerative disorders. Understanding the subtype selectivity …

Emerging approaches to GPCR ligand screening for drug discovery

P Kumari, E Ghosh, AK Shukla - Trends in Molecular Medicine, 2015 - cell.com
The superfamily of G-protein-coupled receptors (GPCRs) represents the largest class of cell
surface receptors and, thus, a prominent family of drug targets. Recently, there has been …

Metabotropic glutamate receptors in Alzheimer's disease synaptic dysfunction: Therapeutic opportunities and hope for the future

A Srivastava, B Das, AY Yao… - Journal of Alzheimer's …, 2020 - content.iospress.com
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by the presence of
neuritic plaques and neurofibrillary tangles. The impaired synaptic plasticity and dendritic …

Hydration and dynamics of l-glutamate ion in aqueous solution

S Friesen, MV Fedotova, SE Kruchinin… - Physical Chemistry …, 2021 - pubs.rsc.org
Aqueous solutions of sodium L-glutamate (NaGlu) in the concentration range 0< c/M≤ 1.90
at 25° C were investigated by dielectric relaxation spectroscopy (DRS) and statistical …