Search Results - "Mayer, Stanislas"

817 DT095895, a selective EP4 receptor antagonist with monotherapy efficacy in syngeneic mouse model(s) and best-in-class properties by Blayo, Anne-Laure, Deshons, Laurène, Dumont, Alexia, Franchet, Christel, Halter, Célia, Herbin, Ludovic, Hommet, Gaël, Mayer, Stanislas, Bessede, Alban, Nafia, Imane, Sidhoum, Marjorie, Leroy, Xavier, Schann, Stéphan

“…BackgroundElevated levels of Prostaglandin E2 (PGE2), an eicosanoid notably synthesized by the cyclooxygenase-2 (COX-2), exert strong immunosuppressive effects…”
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Pd-PEPPSI-IPent super(Cl): A Useful Catalyst for the Coupling of 2-Aminopyridine Derivatives by Khadra, Abir, Mayer, Stanislas, Organ, Michael G

“…The Pd-PEPPSI-IPent super(Cl) precatalyst (PEPPSI=pyridine-enhanced precatalyst preparation stabilisation initiation) has been demonstrated to be highly…”
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A General Protocol for the Broad-Spectrum Cross-Coupling of Nonactivated Sterically Hindered 1° and 2° Amines by Khadra, Abir, Mayer, Stanislas, Mitchell, David, Rodriguez, Michael J, Organ, Michael G

“…While notable advances have been reported for the metal-catalyzed cross-coupling of bulky amines, to date no set of reported conditions has proven general for…”
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Pd‐PEPPSI‐IPentCl: A Useful Catalyst for the Coupling of 2‐Aminopyridine Derivatives by Khadra, Abir, Mayer, Stanislas, Organ, Michael G.

“…The Pd‐PEPPSI‐IPentCl precatalyst (PEPPSI=pyridine‐enhanced precatalyst preparation stabilisation initiation) has been demonstrated to be highly effective in…”
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Pd-PEPPSI-IPent Cl : A Useful Catalyst for the Coupling of 2-Aminopyridine Derivatives by Khadra, Abir, Mayer, Stanislas, Organ, Michael G

“…The Pd-PEPPSI-IPent precatalyst (PEPPSI=pyridine-enhanced precatalyst preparation stabilisation initiation) has been demonstrated to be highly effective in the…”
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Abstract 6697: DT095895, a selective EP4 receptor antagonist with monotherapy efficacy in syngeneic mouse model(s) and best-in-class properties by Blayo, Anne-Laure, Deshons, Laurène, Dumont, Alexia, Franchet, Christel, Halter, Célia, Herbin, Ludovic, Hommet, Gaël, Mayer, Stanislas, Bessede, Alban, Nafia, Imane, Sidhoum, Marjorie, Leroy, Xavier, Schann, Stephan

“…Elevated levels of Prostaglandin E2 (PGE2), an eicosanoid notably synthesized by the cyclooxygenase-2 (COX-2), exert strong immunosuppressive effects in the…”
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Discovery, Structure–Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 by Charvin, Delphine, Pomel, Vincent, Ortiz, Millan, Frauli, Mélanie, Scheffler, Sophie, Steinberg, Edith, Baron, Luc, Deshons, Laurène, Rudigier, Rachel, Thiarc, Delphine, Morice, Christophe, Manteau, Baptiste, Mayer, Stanislas, Graham, Danielle, Giethlen, Bruno, Brugger, Nadia, Hédou, Gaël, Conquet, François, Schann, Stephan

“…The metabotropic glutamate receptor 4 (mGluR4) is an emerging target for the treatment of Parkinson’s disease (PD). However, since the discovery of its…”
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Discovery of BI-9508, a Brain-Penetrant GPR88-Receptor-Agonist Tool Compound for In Vivo Mouse Studies by Fer, Mickael, Amalric, Camille, Arban, Roberto, Baron, Luc, Ben Hamida, Sami, Breh-Schlanser, Petra, Cui, Yunhai, Darcq, Emmanuel, Eickmeier, Christian, Faye, Vincent, Franchet, Christel, Frauli, Mélanie, Halter, Célia, Heyer, Marjorie, Hoenke, Christoph, Hoerer, Stefan, Hucke, Oliver T., Joseph, Christophe, Kieffer, Brigitte L., Lebrun, Louison, Lotz, Noémie, Mayer, Stanislas, Omrani, Azar, Recolet, Mandy, Schaeffer, Laurent, Schann, Stephan, Schlecker, Annette, Steinberg, Edith, Viloria, Mélanie, Würstle, Klaus, Young, Kyle, Zinser, Alexander, Montel, Florian, Klepp, Julian

“…Decreased activity and expression of the G-protein coupled receptor GPR88 is linked to many behavior-linked neurological disorders. Published preclinical GPR88…”
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High-Throughput Screening of Transient Receptor Potential Channel 1 Ligands in the Light of the Bioluminescence Resonance Energy Transfer Technique by Chappe, Yann, Michel, Pauline, Joushomme, Alexandre, Barbeau, Solène, Pierredon, Sandra, Baron, Luc, Garenne, André, Poulletier De Gannes, Florence, Hurtier, Annabelle, Mayer, Stanislas, Lagroye, Isabelle, Quignard, Jean-François, Ducret, Thomas, Compan, Vincent, Franchet, Christelle, Percherancier, Yann

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Regioselective Formylation of Ethyl 3,4-Dihydro-2H-1,4- benzoxazine-2-carboxylate or 2-Acetate Derivatives by Mérour, Jean-Yves, Mayer, Stanislas, Guillaumet, Gérald

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High-Throughput Screening of TRPV1 Ligands in the Light of the Bioluminescence Resonance Energy Transfer Technique by Chappe, Yann, Michel, Pauline, Joushomme, Alexandre, Barbeau, Solène, Pierredon, Sandra, Baron, Luc, Garenne, André, Poulletier De Gannes, Florence, Hurtier, Annabelle, Mayer, Stanislas, Lagroye, Isabelle, Quignard, Jean-François, Ducret, Thomas, Compan, Vincent, Franchet, Christelle, Percherancier, Yann

“…Ion channels are attractive drug targets for many therapeutic applications. However, high-throughput screening (HTS) of drug candidates is difficult and…”
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Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005 - present) by Celanire, Sylvain, Sebhat, Iyassu, Wichmann, Juergen, Mayer, Stanislas, Schann, Stephan, Gatti, Silvia

“…This review focuses on the medicinal chemistry efforts directed toward the identification of competitive and noncompetitive antagonists of glutamate at group…”
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Chemical Switch of a Metabotropic Glutamate Receptor 2 Silent Allosteric Modulator into Dual Metabotropic Glutamate Receptor 2/3 Negative/Positive Allosteric Modulators by Schann, Stephan, Mayer, Stanislas, Franchet, Christel, Frauli, Mélanie, Steinberg, Edith, Thomas, Mireille, Baron, Luc, Neuville, Pascal

“…Using an mGluR2 FRET-based binding assay, binders of the transmembrane region devoid of functional activity were identified. It is reported that slight…”
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HGG-23. GLUTAMINOLYSIS INVOLVEMENT AND ITS TARGETING IN PEDIATRIC HIGH GRADE GLIOMAS: A NEW WAY OF TREATMENT by Fuchs, Quentin, Frauli, Mélanie, Ruhland, Elisa, Keime, Celine, Mayer, Stanislas, Namer, Izzie Jacques, Schann, Stephane, Dontenwill, Monique, Entz-Werlé, Natacha

“…Abstract Gliomas are the most common type of pediatric brain tumors. One third of them are high grade gliomas (pHGG) with a significant dismal prognosis and a…”
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Abstract 684: DT-9045, a novel PAR2 inhibitor with best-in-class properties that reduces resistance to both EGFR-targeting therapies and immunotherapy in oncology models by Brugat, Thibaut, Kadiri, Maleck, Aouad, Samya, Blayo, Anne-Laure, Rugeri, Baptiste, Mousson, Antoine, Janvier, Aurélie, Steinberg, Edith, Baron, Luc, Recolet, Mandy, Wirth, Xavier, Garcia-Leon, Maria Jesus, Ruet, Quentin, Semache, Meriem, Sabbagh, Laurent, Blanchard, Orphée, Franchet, Christel, Mayer, Stanislas, Stagg, John, Lenne, Nathalie, Schann, Stephan

“…Protease-activated receptor 2 (PAR2) is a promising therapeutic target in oncology and immuno-oncology. It is upregulated and associated with poor prognosis in…”
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Abstract 4961: Novel biased PAR2 inhibitors with best-in-class properties reduce resistance to both chemotherapy and immunotherapy in oncology models by Brugat, Thibaut, Bergami, Francesco, Rugeri, Baptiste, Janvier, Aurélie, Steinberg, Edith, Baron, Luc, Recolet, Mandy, Wirth, Xavier, Semache, Meriem, Mousson, Antoine, Dietsch, Camille, Ruet, Quentin, Blanchard, Orphée, Jacoberger-Foissac, Célia, Cousineau, Isabelle, Kadiri, Maleck, Blayo, Anne-Laure, Franchet, Christel, Mayer, Stanislas, Stagg, John, Lenne, Nathalie, Schann, Stephan

“…A large-scale meta-analysis has recently identified Protease-activated receptor 2 (PAR2) gene expression to be significantly associated with resistance to…”
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Synthesis of 4-(5-Iodo-3-Methylpyrazolyl) Phenylsulfonamide and Its Elaboration To a COX II Inhibitor Library by Solution-Phase Suzuki Coupling Using Pd/C as a Solid-Supported Catalyst by Organ, Michael G, Mayer, Stanislas

“…An effective synthesis of 4-(5-iodo-3-methylpyrazolyl) phenylsulfonamide has been developed. This aromatic iodide template served as an efficient oxidative…”
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Screening of Inhibitors Using Enzymes Entrapped in Sol−Gel-Derived Materials by Besanger, Travis R, Chen, Yang, Deisingh, Anil K, Hodgson, Richard, Jin, Wen, Mayer, Stanislas, Brook, Michael A, Brennan, John D

“…In recent years, a number of new methods have been reported that make use of immobilized enzymes either on microarrays or in bioaffinity columns for…”
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A 2.13 Å Structure of E. coli Dihydrofolate Reductase Bound to a Novel Competitive Inhibitor Reveals a New Binding Surface Involving the M20 Loop Region by Summerfield, Rachael L, Daigle, Denis M, Mayer, Stanislas, Mallik, Debasis, Hughes, Donald W, Jackson, Sean G, Sulek, Margaret, Organ, Michael G, Brown, Eric D, Junop, Murray S

“…Dihydrofolate reductase (DHFR) is a vital metabolic enzyme and thus a clinically prominent target in the design of antimetabolites. In this work, we identify…”
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Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): Identification of a new group III metabotropic glutamate receptor selective agonist by Schann, Stephan, Menet, Christel, Arvault, Paul, Mercier, Géraldine, Frauli, Mélanie, Mayer, Stanislas, Hubert, Nadia, Triballeau, Nicolas, Bertrand, Hugues-Olivier, Acher, Francine, Neuville, Pascal

“…A new family of mGlu receptor orthosteric ligands called APTCs was designed and synthesized using parallel chemistry. Amongst them, 8a06 (FP0429) has been…”
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