Výsledky vyhledávání - "Michelle A. Uberti"

Discovery and structure–activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators

Autor: Dario Doller, Guiying Li, Hermogenes N. Jimenez, Robbin Brodbeck, Michelle A. Uberti, Daniel G. Smith, Hao Zhou, Jens Christian Madsen, Henrik Pedersen, Michel Grenon, Gamini Chandrasena, Sidney W. Topiol

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:1398-1406

A novel series of trans-1,3-cyclohexyl diamides was discovered and characterized as mGluR5 negative allosteric modulators (NAMs) lacking an alkyne moiety. Conformational constraint of one of the amide bonds in the diamide template led to a spirooxazo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6ab971983d6dcff5223bdaed66c13e9
https://doi.org/10.1016/j.bmcl.2012.12.078

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4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators

Autor: Manuel Cajina, Megan Nattini, Michael Sabio, Michael S. Reitman, Dario Doller, Kevin G. Liu, Maria D. Bacolod, Hermogenes N. Jimenez, Sang-Phyo Hong, Michelle A. Uberti

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:3235-3239

4-(1-Phenyl-1H-pyrazol-4-yl)quinoline (1) was identified by screening the Lundbeck compound collection, and characterized as having mGlu4 receptor positive allosteric modulator properties. Compound 1 is selective over other mGlu receptors and a panel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b69b52a2908d3eaca5c8afd4f35dc6a
https://doi.org/10.1016/j.bmcl.2012.03.032

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Structure-Activity Relationships for Negative Allosteric mGluR5 Modulators

Autor: Søren Møller Nielsen, Hans Bräuner-Osborne, Ulf Madsen, Trine Kvist, Birgitte H. Kaae, Birgitte Nielsen, Hermogenes N. Jimenez, Kasper Harpsøe, Rasmus P. Clausen, Christina Mølck, Michelle A. Uberti, David E. Gloriam, Jesper Mosolff Mathiesen, Per Sauerberg

Publikováno v: ChemMedChem. 7:440-451

A series of compounds based on the mGluR5-selective ligand 2-methyl-6-(phenylethynyl)pyridine (MPEP) were designed and synthesized. The compounds were found to be either structural analogues of MPEP, substituted monomers, or dimeric analogues. All co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7774d86454abd58c47505cdaa9660566
https://doi.org/10.1002/cmdc.201100578

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Development of an Aequorin Luminescence Calcium Assay for High-Throughput Screening Using a Plate Reader, the LumiLux

Autor: Poda Suresh Babu, Michelle A. Uberti, Arun Ranganathn, Michael Sabio, Claus T. Christoffersen, Veena Menon, Vincent H. Jorgensen, Kenneth A. Jones

Publikováno v: ASSAY and Drug Development Technologies. 6:787-794

A luminescence assay using a new plate reader, the LumiLux (PerkinElmer, Waltham, MA), has been validated for high-throughput screening (HTS). In this study, we compared the aequorin luminescence-based calcium mobilization assay to the fluorescence-b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b2671105a552d9b37d214aa7192ea90
https://doi.org/10.1089/adt.2008.157

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Olfactory receptor surface expression is driven by association with the β 2 -adrenergic receptor

Autor: Cristina F. Bush, Randy A. Hall, Kerry J. Ressler, Seth V. Jones, Chris Hague, Kenneth P. Minneman, Michelle A. Uberti, Zhongjian Chen

Publikováno v: Proceedings of the National Academy of Sciences. 101:13672-13676

Olfactory receptors (ORs) comprise more than half of the large class I G protein-coupled receptor (GPCR) superfamily. Although cloned over a decade ago, little is known about their properties because wild-type ORs do not efficiently reach the cell su

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a6e187fe43ec7433d37da2460baccc6
https://doi.org/10.1073/pnas.0403854101

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Cell Surface Expression of α1D-Adrenergic Receptors Is Controlled by Heterodimerization with α1B-Adrenergic Receptors

Autor: Michelle A. Uberti, Kenneth P. Minneman, Randy A. Hall, Chris Hague, Zhongjian Chen

Publikováno v: Journal of Biological Chemistry. 279:15541-15549

alpha(1)-Adrenergic receptors (ARs) belong to the large Class I G protein-coupled receptor superfamily and comprise three subtypes (alpha(1A), alpha(1B), and alpha(1D)). Previous work with heterologously expressed C-terminal green fluorescent protein

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93c674487eec1693f1c5b64e4a56332e
https://doi.org/10.1074/jbc.m314014200

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Molecular characterization of a rabbit long-chain fatty acyl CoA synthetase that is highly expressed in the vascular endothelium

Autor: Michelle A Uberti, James C. Pierce, Margaret T. Weis

Publikováno v: Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1645:193-204

The formation of coenzyme A thioesters from long-chain fatty acids represents a metabolic branch point. We have isolated, cloned and sequenced a long-chain fatty acyl CoA synthetase (LCFACoAS) that is localized to the endothelium of rabbit heart and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::388e444af97fee65cc102afa917fb60e
https://doi.org/10.1016/s1570-9639(02)00540-x

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Biochemistry and Pharmacology of Epitope-Tagged α1-Adrenergic Receptor Subtypes

Autor: George A. Rogge, Aleksandra Vicentic, Michelle A. Uberti, Anna Robeva, Kenneth P. Minneman

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 302:58-65

Human alpha(1A)-, alpha(1B)-, and alpha(1D)-adrenergic receptors were tagged at their amino termini with FLAG epitopes and stably expressed in human embryonic kidney (HEK)293 cells. Tagged receptors demonstrated a wild-type pharmacology and mobilizat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ae0421064c39bb12b47629676f7794e
https://doi.org/10.1124/jpet.302.1.58

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Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu4 receptor

Autor: Michelle A. Uberti, Agnieszka Pałucha-Poniewiera, Katarzyna Stachowicz, Dario Doller, Maria A. Bacolod, Joanna M. Wierońska, Andrzej Pilc, Anna Sławińska

Previous studies demonstrated that the Group III mGlu receptor-selective orthosteric agonist, LSP1-2111 produced anxiolytic- but not antidepressant-like effects upon peripheral administration. Herein, we report the pharmacological actions of Lu AF219

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e3f22faaea2cc80e718056d9be38414
https://ruj.uj.edu.pl/xmlui/handle/item/97567

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Synergy between L-DOPA and a novel positive allosteric modulator of metabotropic glutamate receptor 4: implications for Parkinson's disease treatment and dyskinesia

Autor: Lydia Kerkerian-Le Goff, Dario Doller, Christophe Melon, Khaled-Ezaheir Bennouar, Maria D. Bacolod, Hermogenes N. Jimenez, Paolo Gubellini, Manuel Cajina, Michelle A. Uberti

Publikováno v: Neuropharmacology
Neuropharmacology, 2013, 66, pp.158-69. ⟨10.1016/j.neuropharm.2012.03.022⟩
Neuropharmacology, Elsevier, 2013, 66, pp.158-69. ⟨10.1016/j.neuropharm.2012.03.022⟩

Group III metabotropic glutamate (mGlu) receptors are localized in presynaptic terminals within basal ganglia (BG) circuitry that become hyperactive due to dopamine depletion in Parkinson's disease (PD). For this reason, group III mGlu receptors, in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::130c4170b8541db9c1b59a920fbb96ba
https://pubmed.ncbi.nlm.nih.gov/22491024

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