Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Mark H. Pausch"'
Autor:
Christina N. DiMarco, Anthony L. Gotter, Alan T. Savitz, Joanne Stevens, Joseph G. Bruno, Tamara D. Cabalu, John J. Renger, Jason W. Skudlarek, Pamela L. Tannenbaum, Paul J. Coleman, Scott D. Kuduk, Joseph Brunner, Susan L. Garson, Christopher J. Winrow, Julie A. O'Brien, Charles M. Harrell, Mark H. Pausch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2488-2492
Antagonism of orexin receptors has shown clinical efficacy as a novel paradigm for the treatment of insomnia and related disorders. Herein, molecules related to the dual orexin receptor antagonist filorexant were transformed into compounds that were
Autor:
Steven M. Grauer, Peter J. Atkinson, Michael A. Olsen, Cody Kelley, Deborah L. Smith, Margaret Lai, Guoming Zhang, Feng Liu, Sharon Rosenzweig-Lipson, Chad E. Beyer, Michael Popiolek, Adam M. Gilbert, Mark Day, Karen L. Marquis, Radka Graf, Rachel Navarra, Claudine Pulicicchio, Farhana Pruthi, Xavier Z. Khawaja, Evguenia Kouranova, Sheree F. Logue, Tom A. Comery, Caitlin Wantuch, Mark H. Pausch, Nicholas J. Brandon
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 327:827-839
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor subtype 5 (mGlu5) enhance N-methyl-d-aspartate receptor function and may represent a novel approach for the treatment of schizophrenia. ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fl
Autor:
Eugene Tseng, Ying Sun, Maria Blatcher, Jeremy Johnson, Lynn Zhang, Noel Taylor, Sreekumar Raman Kodangattil, Janet E. Paulsen, Stan P. Nawoschik, Brian Bates, David C. Kopsco, Angela Kramer, Hui Min Chen, Qin Shan, Mark H. Pausch
Publikováno v:
Brain Research. 1087:1-14
This report describes the identification and characterization of the murine orphan GPCR, Gpr101. Both human and murine genes were localized to chromosome X. Similar to its human ortholog, murine Gpr101 mRNA was detected predominantly in the brain wit
Publikováno v:
Bioinformatics. 20:3490-3499
Motivation: Determining the coupling specificity of G-protein coupled receptors (GPCRs) is important for understanding the biology of this class of pharmacologically important proteins. Currently available in silico methods for predicting GPCR–G-pr
Publikováno v:
Journal of Biological Chemistry. 278:47466-47476
G protein-coupled receptor kinases (GRKs) specifically bind and phosphorylate the agonist-occupied form of G protein-coupled receptors. To further characterize the mechanism of GRK/receptor interaction, we developed a yeast-based bioassay using strai
Publikováno v:
Journal of Neurochemistry. 77:1327-1337
The goal of this study was to functionally express the three G(q)-coupled muscarinic receptor subtypes, M(1), M(3) and M(5), in yeast (Saccharomyces cerevisiae). Transformation of yeast with expression constructs coding for the full-length receptors
Autor:
Danielle Raufaste, Clarice Schmidt, Mark H. Pausch, Evi Kostenis, Claudine Serradeil-Le Gal, Jürgen Wess, Mark E. Dumont, Isolde Erlenbach
Publikováno v:
Journal of Biological Chemistry. 276:29382-29392
To facilitate structure-function relationship studies of the V2 vasopressin receptor, a prototypical G(s)-coupled receptor, we generated V2 receptor-expressing yeast strains (Saccharomyces cerevisiae) that required arginine vasopressin-dependent rece
Publikováno v:
Molecular and Cellular Biology. 15:6188-6195
A detailed analysis of structural and functional aspects of G-protein-coupled receptors, as well as discovery of novel pharmacophores that exert their effects on members of this class of receptors, will be facilitated by development of a yeast-based
Autor:
Pranab K. Chanda, Eckart D. Gundelfinger, John F. Ross, Stephen J. Moss, Mark H. Pausch, Michael Popiolek, Erik I. Charych, Nicholas J. Brandon
Publikováno v:
The Journal of biological chemistry. 286(33)
Schizophrenia is a highly heritable neuropsychiatric disorder affecting ∼1% of the world's population. Linkage and association studies have identified multiple candidate schizophrenia susceptibility genes whose functions converge on the glutamaterg
Autor:
Jean Zhang, Ping Zhou, Tikva Carrick, Albert J. Robichaud, Rolf Feenstra, Jan-Hendrik Reinders, Dianne Kowal, Chris G. Kruse, Martina A.W. van der Neut, Yinfa Yan, David P. Rotella, Mark H. Pausch, Margaret Lai, Karen L. Marquis
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(9)
A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D2 ligands to prepare a series of dual acting compounds with attractive in vitr