Virtual screening workflow development guided by the “receiver operating characteristic” curve approach. Application to high-throughput docking on metabotropic …

N Triballeau, F Acher, I Brabet, JP Pin… - Journal of medicinal …, 2005 - ACS Publications
The “receiver operating characteristic” (ROC) curve method is a well-recognized metric
used as an objective way to evaluate the ability of a given test to discriminate between two …

The metabotropic glutamate receptors: structure, activation mechanism and pharmacology

JP Pin, F Acher - Current Drug Targets-CNS & Neurological …, 2002 - ingentaconnect.com
The metabotropic glutamate receptors are G-protein coupled receptors (GPCR) involved in
the regulation of many synapses, including most glutamatergic fast excitatory synapses. Eight …

[HTML][HTML] The heptahelical domain of GABAB2 is activated directly by CGP7930, a positive allosteric modulator of the GABAB receptor

V Binet, C Brajon, L Le Corre, F Acher, JP Pin… - Journal of Biological …, 2004 - ASBMB
The γ-aminobutyric acid, type B (GABA B ) receptor is well recognized as being composed
of two subunits, GABA B1 and GABA B2 . Both subunits share structural homology with other …

Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors

…, J Liu, M Cohen-Gonsaud, F Acher… - Proceedings of the …, 2004 - National Acad Sciences
Although agonists bind directly in the heptahelical domain (HD) of most class-I rhodopsin-like
G protein coupled receptors (GPCRs), class-III agonists bind in the extracellular domain of …

Electrophysiological and behavioral evidence that modulation of metabotropic glutamate receptor 4 with a new agonist reverses experimental parkinsonism

…, P Gubellini, L Kerkerian-LeGoff, F Acher… - The FASEB …, 2009 - Wiley Online Library
Developing nondopaminergic palliative treatments for Parkinson's disease represents a
major challenge to avoid the debilitating side effects produced by l‐DOPA therapy. Increasing …

Comparative effect of L-CCG-I, DCG-IV and γ-carboxy-L-glutamate on all cloned metabotropic glutamate receptor subtypes

…, ML Parmentier, C De Colle, J Bockaert, F Acher… - …, 1998 - Elsevier
In a previous study we reported that the addition of a carboxylic group to the mGlu receptor
agonist aminocyclopentane-1,3-dicarboxylate (ACPD) changes its properties from agonist to …

Group III metabotropic glutamate receptors inhibit hyperalgesia in animal models of inflammation and neuropathic pain

C Goudet, E Chapuy, A Alloui, F Acher, JP Pin… - Pain, 2008 - journals.lww.com
Glutamate plays a key role in modulation of nociceptive processing. This excitatory amino
acid exerts its action through two distinct types of receptors, ionotropic and metabotropic …

[HTML][HTML] Asymmetric functioning of dimeric metabotropic glutamate receptors disclosed by positive allosteric modulators

…, V Hlavackova, F Malhaire, D Maurel, F Acher… - Journal of Biological …, 2005 - ASBMB
The recent discovery of positive allosteric modulators (PAMs) for G-protein-coupled receptors
open new possibilities to control a number of physiological and pathological processes. …

New perspectives for the development of selective metabotropic glutamate receptor ligands

JP Pin, C De Colle, AS Bessis, F Acher - European journal of pharmacology, 1999 - Elsevier
The metabotropic glutamate receptors are GTP-binding-protein (G-protein) coupled receptors
that play important roles in regulating the activity of many synapses in the central nervous …

A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential

…, H McLean, H Daniel, M Amalric, F Acher… - The FASEB …, 2012 - Wiley Online Library
Metabotropic glutamate (mGlu) receptors are promising targets to treat numerous brain
disorders. So far, allosteric modulators are the only subtype selective ligands, but pure agonists …