Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Emmanuel Le Poul"'
Autor:
Jacob Raber, Matthew J. Davis, Isabelle Royer-Urios, Christelle Bolea, Simon T. Bate, Susan E. Browne, Brice Campo, Francoise Girard, Massimiliano Fonsi, Sylvain Celanire, Jason M. Uslaner, Robert M. Duvoisin, Mikhail Kalinichev, Ian J. Reynolds, Sonia Poli, Emmanuel Le Poul
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 350:495-505
There is growing evidence that activation of metabotropic glutamate receptor 4 (mGlu4) leads to anxiolytic- and antipsychotic-like efficacy in rodent models, yet its relevance to depression-like reactivity remains unclear. Here, we present the pharma
Autor:
Si Qin, Mark Epping-Jordan, David A. Kendall, Charles A. Marsden, Ben H.C. Westerink, David E. Ray, Emmanuel Le Poul, Kevin C. F. Fone, Nektaria Papadopoulou, Nisha Kurian, Tyson V. Sharp, Madeleine V. King, Thomas I. F. H. Cremers
Publikováno v:
Neuropsychopharmacology, 39(2), 464-476. Nature Publishing Group
Glutamate is the principle excitatory neurotransmitter in the mammalian brain, and dysregulation of glutamatergic neurotransmission is implicated in the pathophysiology of several psychiatric and neurological diseases. This study utilized novel lenti
Autor:
Robert Johannes Lütjens, Vincent Mutel, Bernard Ludwig, Beatrice Bonnet, Jean-Philippe Rocher, Emmanuel Le Poul, Christelle Bolea, Mark Epping-Jordan, Bessis Anne-Sophie, Sonia Poli
Publikováno v:
Current Topics in Medicinal Chemistry. 11:680-695
Allosteric modulators of metabotropic glutamate receptors (mGluR) subtypes 1-8 have been shown to offer a valid way to develop small molecule non aminoacid-like therapeutics that can be administered orally and that readily cross the blood-brain barri
Autor:
Robert Johannes Lütjens, Andrés A. Trabanco, Vanthea Nhem, Yves Thollon, Géraldine Poulain, Philippe Cluzeau, Rocco Furnari, Jean-Philippe Rocher, Nadia Behaj, Gregor James Macdonald, Hassan Julien Imogai, Hilde Lavreysen, José María Cid, Terry Patrick Finn, Nicolas Poirier, Sonia Poli, Emmanuel Le Poul, David D’Addona, José Ignacio Andrés, Alexandre Raux, Guillaume Albert Jacques Duvey
Publikováno v:
MedChemComm. 2:132-139
A series of N-propyl-5-substituted isoquinolones was identified as positive allosteric modulators (PAM) of metabotropic glutamate receptor 2 (mGluR2) via high-throughput screening (HTS). The subsequent synthesis and preliminary SAR exploration that l
Autor:
Philippe Cluzeau, Hassan Julien Imogai, Mark Epping-Jordan, Alexandre Raux, Guillaume Albert Jacques Duvey, Jean-Philippe Rocher, Gregor James Macdonald, José María Cid, Ana Isabel de Lucas, Juan Antonio Vega, Vanthea Nhem, Francis Derouet, Gary Tresadern, Andrés A. Trabanco, Christelle Boléa, José Ignacio Andrés, Robert Johannes Lütjens, Daniel Oehlrich, Karim Macary, Encarnación Matesanz, Hilde Lavreysen, Terry Patrick Finn, Sonia Poli, Jessica Muller, María Lourdes Linares, Nicolas Poirier, Francoise Girard, Julen Oyarzabal, Emilie Chamelot, Emmanuel Le Poul
Publikováno v:
ACS Chemical Neuroscience. 1:788-795
The discovery and characterization of compound 48, a selective and in vivo active mGlu2 receptor positive allosteric modulator (PAM), are described. A key to the discovery was the rational exploration of the initial HTS hit 13 guided by an overlay mo
Autor:
Françoise Bachelerie, Sébastien Ballet, Thierry Planchenault, Cédric Blanpain, Marc Parmentier, Bernard Lagane, Karl Balabanian, Yann Percherancier, Martin Oppermann, Gilbert Vassart, Isabelle Staropoli, Emmanuel Le Poul
Publikováno v:
Molecular Pharmacology. 67:1966-1976
CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor that governs migration of leukocytes and serves as a coreceptor for the R5 tropic strains of human immunodeficiency virus (HIV). CCR5-mediated signaling in response to CC chemokines relie
Autor:
Alberto Mantovani, Marisa Vulcano, Cédric Blanpain, Gilbert Vassart, Isabelle Migeotte, Valérie Wittamer, David Communi, Jean-Denis Franssen, Stéphane Brézillon, Silvano Sozzani, Jean François Mirjolet, Marc Parmentier, Richard Tyldesley, Michel Detheux, Emmanuel Le Poul
Publikováno v:
The Journal of Experimental Medicine, 198 (7
The Journal of Experimental Medicine
The Journal of Experimental Medicine
Dendritic cells (DCs) and macrophages are professional antigen-presenting cells (APCs) that play key roles in both innate and adaptive immunity. ChemR23 is an orphan G protein-coupled receptor related to chemokine receptors, which is expressed specif
Autor:
Cecile Loison, Marc Parmentier, Stéphane Brézillon, Gilbert Vassart, Jean-Yves Springael, Vincent Lannoy, Michel Detheux, Vincent Dupriez, Emmanuel Le Poul, Sofie Struyf, Jozef Van Damme, Marie-Eve Decobecq
Publikováno v:
Journal of Biological Chemistry. 278:25481-25489
Short chain fatty acids (SCFAs), including acetate, propionate, and butyrate, are produced at high concentration by bacteria in the gut and subsequently released in the bloodstream. Basal acetate concentrations in the blood (about 100 microm) can fur
Autor:
Jean Lucchetti, Emmanuel Le Poul, Vincent Dupriez, Stéphane Brézillon, Michel Detheux, Jean-Denis Franssen, Marc Parmentier, Vincent Lannoy
Publikováno v:
Journal of Biological Chemistry. 278:776-783
GPR7 and GPR8 are two structurally related orphan G protein-coupled receptors, presenting high similarities with opioid and somatostatin receptors. Two peptides, L8 and L8C, derived from a larger precursor, were recently described as natural ligands
Autor:
Vincent Dupriez, Yoshinori Mizuguchi, Emmanuel Le Poul, Michel Detheux, Emmanuel Burgeon, Sunao Hisada
Publikováno v:
SLAS Discovery. 7:57-65
AequoScreen, a cellular aequorin-based functional assay, has been optimized for luminescent high-throughput screening (HTS) of G protein-coupled receptor (GPCRs). AequoScreen is a homogeneous assay in which the cells are loaded with the apoaequorin c