Výsledky vyhledávání - "Magalie, Rocheville"

An industrial perspective on positive allosteric modulation as a means to discover safe and selective drugs

Autor: Stephen L. Garland, Magalie Rocheville

Publikováno v: Drug Discovery Today: Technologies. 7:e87-e94

Positive allosteric modulation is an innovative strategy for the discovery of drugs acting at 7-transmembrane receptors. Screening has led to the identification of numerous starting points for medicinal chemistry typified by novel mechanisms of actio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87715496d2a76ab5751a7504b4b73de6
https://doi.org/10.1016/j.ddtec.2010.06.004

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The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2

Autor: Stephen P. Watson, Adelheid Roth, Anna Sava, Greg J. Osborne, David John Nash, Paloma Perez, Ben Powney, Corrado Corti, Magalie Rocheville, Paul W. Smith, Clive Leslie Branch, Federica Bianchi, Pier D’Alessandro, Emma Koppe, Maite de los Frailes, Jesús Ángel de la Fuente, Annarosa Ugolini, Dino Montanari, Stephen L. Garland

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:759-762

The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described. Structure-activity relationships, attenuation of dopamine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5af6d59aa839fa93266ba75cb6cf3fc
https://doi.org/10.1016/j.bmcl.2009.11.032

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Evaluation of the mGlu8 receptor as a putative therapeutic target in schizophrenia

Autor: James N.C. Kew, Peter R. Maycox, Ellen M. Soffin, Rosemary A. Melarange, Andrew Jonathan Harris, Melanie J. Robbins, Claire Rourke, Jay Strum, Fiona M. Kelly, Magalie Rocheville, Gareth A. Jones, Declan N.C. Jones, Paul R. Murdock, Tom Rupniak, Andy Honey, Kathryn R. Starr

Publikováno v: Brain Research. 1152:215-227

Aberrant glutamatergic neurotransmission may underlie the pathogenesis of schizophrenia and metabotropic glutamate receptors (mGluRs) have been implicated in the disease. We have established the localization of the group III mGluR subtype, mGluR8, in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1281b827d16319258572c1d22e0e1b25
https://doi.org/10.1016/j.brainres.2007.03.028

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The Cytoplasmic Tail of the Human Somatostatin Receptor Type 5 Is Crucial for Interaction with Adenylyl Cyclase and in Mediating Desensitization and Internalization

Autor: Yogesh C. Patel, Nedim Hukovic, Rosemarie Panetta, Ujendra Kumar, Magalie Rocheville

Publikováno v: Journal of Biological Chemistry. 273:21416-21422

We have investigated the role of the cytoplasmic tail (C-tail) of the human somatostatin receptor type 5 (hSSTR5) in regulating receptor coupling to adenylyl cyclase (AC) and in mediating agonist-dependent desensitization and internalization response

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c4af2d8be47c8fbe19057ab59e7b802
https://doi.org/10.1074/jbc.273.33.21416

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Mining the potential of label-free biosensors for seven-transmembrane receptor drug discovery

Autor: Magalie, Rocheville, Julio, Martin, Jeff, Jerman, Evi, Kostenis

Publikováno v: Progress in molecular biology and translational science. 115

Label-free is a broad term used to describe a number of cutting-edge biosensor technologies that have attracted considerable attention in the area of drug discovery for seven-transmembrane G protein-coupled receptors (GPCRs). Label-free biosensors re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::867cd137e5813420804d06fcd7dc6e39
https://pubmed.ncbi.nlm.nih.gov/23415093

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In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

Autor: M. H. Selina Mok, Laura Zonzini, Laurie J. Gordon, Vivian J A Costantini, Massimo Gianotti, Enzo Valerio, Magalie Rocheville, Corrado Carignani, Elisabetta Perdona, Mauro Corsi, Prisca Martinelli, Filippo Visentini, Anna Maria Capelli, Michela Tessari

Publikováno v: Neuropharmacology. 61(5-6)

There is preclinical evidence supporting the finding that the GABA(B) receptor orthosteric agonist, baclofen, has significant effects on eating behavior suggesting the potential therapeutic application of this compound for the treatment of eating rel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fed19595c4ca8b812f610a25373649b
https://pubmed.ncbi.nlm.nih.gov/21756923

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7TM pharmacology measured by label-free: a holistic approach to cell signalling

Autor: Magalie Rocheville, Jeff C. Jerman

Publikováno v: Current opinion in pharmacology. 9(5)

Ligands acting at 7-transmembrane receptors (7TMs) transduce effects on cellular behaviour in a notion termed efficacy; in turn, the cellular behaviour or phenotype can be quantified. Underpinning efficacy is the ability of ligands to dictate the tri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d60233ef0220c3db311a2957516e1c67
https://pubmed.ncbi.nlm.nih.gov/19671497

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Agonist-induced up-regulation of human somatostatin receptor type 1 is regulated by beta-arrestin-1 and requires an essential serine residue in the receptor C-tail

Autor: Ujendra Kumar, Magalie Rocheville, José L. Ramírez, Heather L. Watt

Publikováno v: Biochimica et biophysica acta. 1669(2)

We have previously shown that the human somatostatin receptor type 1 (hSSTR1) does not undergo agonist-induced internalization, but is instead up-regulated at the membrane upon prolonged somatostatin (SST) exposure. The deletion of the carboxytermina

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6478af85f588e6caa07ad01af905004e
https://pubmed.ncbi.nlm.nih.gov/15893521

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Ligand binding to somatostatin receptors induces receptor-specific oligomer formation in live cells

Autor: Magalie Rocheville, Enrico Gratton, Ujendra Kumar, Yogesh C. Patel, Aruna Rani, Don C. Lamb, Shutish C. Patel, John Eid, Theodore L. Hazlett, Michael P. Grant, Ramesh C. Patel

Publikováno v: Patel, RC; Kumar, U; Lamb, DC; Eid, JS; Rocheville, M; Grant, M; et al.(2002). Ligand binding to somatostatin receptors induces receptor-specific oligomer formation in live cells. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 99(5), 3294-3299. doi: 10.1073/pnas.042705099. UC Irvine: Retrieved from: http://www.escholarship.org/uc/item/3s94v8tf

Heptahelical receptors (HHRs) are generally thought to function as monomeric entities. Several HHRs such as somatostatin receptors (SSTRs), however, form homo- and heterooligomers when activated by ligand binding. By using dual fluorescent ligands si

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23e193a4c261beeb6ead206250b2fe76
http://www.escholarship.org/uc/item/3s94v8tf

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