Search Results - "Le Poul, Emmanuel"
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Characterization of an mGluR2/3 Negative Allosteric Modulator in Rodent Models of Depression
Published in Journal of neurogenetics (01-12-2011)“…There is growing evidence suggesting that antagonists of group II metabotropic glutamate receptors (mGluR2/3) exhibit antidepressant-like properties in several…”
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ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization
Published in The Journal of pharmacology and experimental therapeutics (01-03-2013)“…Metabotropic glutamate receptor 7 (mGlu(7)) has been suggested to be a promising novel target for treatment of a range of disorders, including anxiety,…”
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3
Functional Characterization of Human Receptors for Short Chain Fatty Acids and Their Role in Polymorphonuclear Cell Activation
Published in The Journal of biological chemistry (11-07-2003)“…Short chain fatty acids (SCFAs), including acetate, propionate, and butyrate, are produced at high concentration by bacteria in the gut and subsequently…”
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4
Specific recruitment of antigen-presenting cells by chemerin, a novel processed ligand from human inflammatory fluids
Published in The Journal of experimental medicine (06-10-2003)“…Dendritic cells (DCs) and macrophages are professional antigen-presenting cells (APCs) that play key roles in both innate and adaptive immunity. ChemR23 is an…”
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The Metastasis Suppressor Gene KiSS-1 Encodes Kisspeptins, the Natural Ligands of the Orphan G Protein-coupled Receptor GPR54
Published in The Journal of biological chemistry (14-09-2001)“…Natural peptides displaying agonist activity on the orphan G protein-coupled receptor GPR54 were isolated from human placenta. These 54-, 14,- and 13-amino…”
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Pharmacological characterization of the human P2Y13 receptor
Published in Molecular pharmacology (01-07-2003)“…The P2Y13 receptor has recently been identified as a new P2Y receptor sharing a high sequence homology with the P2Y12 receptor as well as similar functional…”
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mGluR5 negative allosteric modulators overview: a medicinal chemistry approach towards a series of novel therapeutic agents
Published in Current topics in medicinal chemistry (01-03-2011)“…Allosteric modulators of metabotropic glutamate receptors (mGluR) subtypes 1-8 have been shown to offer a valid way to develop small molecule non…”
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Supersensitivity of human metabotropic glutamate 1a receptor signaling in L929sA cells
Published in Molecular pharmacology (01-05-2002)“…The effect of antagonist pretreatment on the signaling properties of the human metabotropic glutamate 1a (hmGlu1a) receptor was examined in stably transfected…”
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Pharmacological and pharmacokinetic properties of JNJ‐40411813, a positive allosteric modulator of the mGlu2 receptor
Published in Pharmacology research & perspectives (01-02-2015)“…Compounds modulating metabotropic glutamate type 2 (mGlu2) receptor activity may have therapeutic benefits in treating psychiatric disorders like schizophrenia…”
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10
Identification of Natural Ligands for the Orphan G Protein-coupled Receptors GPR7 and GPR8
Published in The Journal of biological chemistry (10-01-2003)“…GPR7 and GPR8 are two structurally related orphan G protein-coupled receptors, presenting high similarities with opioid and somatostatin receptors. Two…”
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Mutation of the DRY motif reveals different structural requirements for the CC chemokine receptor 5-mediated signaling and receptor endocytosis
Published in Molecular pharmacology (01-06-2005)“…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…”
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New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): Identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones
Published in Bioorganic & medicinal chemistry letters (01-02-2011)“…A series of N-propyl-8-chloro-6-substituted isoquinolones was identified as positive allosteric modulators of metabotropic glutamate receptor 2 (mGluR2 PAM)…”
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13
Multiple active states and oligomerization of CCR5 revealed by functional properties of monoclonal antibodies
Published in Molecular biology of the cell (01-02-2002)“…CC-chemokine receptor 5 (CCR5) is the principal coreceptor for macrophage-tropic strains of human immunodeficiency virus type 1 (HIV-1). We have generated a…”
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Functional characterization of a human receptor for neuropeptide FF and related peptides
Published in British journal of pharmacology (01-05-2001)“…Neuropeptides FF (NPFF) and AF (NPAF) are involved in pain modulation and opioid tolerance. These peptides were known to act through uncharacterized G…”
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Activation of CCR5 by Chemokines Involves an Aromatic Cluster between Transmembrane Helices 2 and 3
Published in The Journal of biological chemistry (17-01-2003)“…CCR5 is a G protein-coupled receptor responding to four natural agonists, the chemokines RANTES (regulated on activation normal T cell expressed and secreted),…”
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Palmitoylation of CCR5 Is Critical for Receptor Trafficking and Efficient Activation of Intracellular Signaling Pathways
Published in The Journal of biological chemistry (29-06-2001)“…CCR5 is a CC chemokine receptor expressed on memory lymphocytes, macrophages, and dendritic cells and also constitutes the main coreceptor for…”
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17
Aequorin-based functional assays for G-protein-coupled receptors, ion channels, and tyrosine kinase receptors
Published in Receptors & channels (01-01-2002)“…Aequorin is a photoprotein originating from jellyfish, whose luminescent activity is dependent on the concentration of calcium ions. Due to the high…”
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A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease
Published in The Journal of pharmacology and experimental therapeutics (01-10-2012)“…Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) have been proposed as a novel therapeutic approach for the treatment of…”
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Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders
Published in The Journal of pharmacology and experimental therapeutics (01-09-2014)“…There is growing evidence that activation of metabotropic glutamate receptor 4 (mGlu4) leads to anxiolytic- and antipsychotic-like efficacy in rodent models,…”
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A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core
Published in Bioorganic & medicinal chemistry letters (15-08-2013)“…A series of potent non-acetylinic negative allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5 NAMs) was developed starting from HTS…”
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