Karen J Gregory

Summary

Affiliation: Vanderbilt University
Country: USA

Publications

  1. ncbi Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential
    Karen J Gregory
    Department of Pharmacology, Vanderbilt Program in Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232 0697, USA
    Neuropharmacology 60:66-81. 2011
  2. ncbi Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships
    Karen J Gregory
    Department of Pharmacology, Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Vanderbilt University Medical Center, Nashville, Tennessee 37232, USA
    Mol Pharmacol 82:860-75. 2012
  3. ncbi Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity
    Jerri M Rook
    Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232 0697, USA
    Biol Psychiatry 73:501-9. 2013
  4. ncbi Allosteric modulation of metabotropic glutamate receptors
    Douglas J Sheffler
    Department of Pharmacology, Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    Adv Pharmacol 62:37-77. 2011
  5. ncbi Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover
    Jason T Manka
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    Bioorg Med Chem Lett 22:6481-5. 2012
  6. ncbi Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders
    Karen J Gregory
    Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    Prog Mol Biol Transl Sci 115:61-121. 2013

Collaborators

  • Shaun R Stauffer
  • Thomas M Bridges
  • Alice L Rodriguez
  • Jens Meiler
  • Craig W Lindsley
  • Jason T Manka
  • Jerri M Rook
  • P Jeffrey Conn
  • Colleen M Niswender
  • Ya Zhou
  • Carrie K Jones
  • Paige N Vinson
  • J Scott Daniels
  • Douglas J Sheffler
  • Hyekyung P Cho
  • Zixiu Xiang
  • Wendy A Pouliot
  • Rocco D Gogliotti
  • Meredith J Noetzel
  • F Edward Dudek
  • Elizabeth J Herman
  • Hilde Lavreysen
  • Gregor J Macdonald
  • Emily Days
  • Richard Williams
  • Satya Jadhav
  • Thomas Steckler
  • Kiran Gogi
  • C David Weaver
  • Claire Mackie
  • José M Bartolomé

Detail Information

Publications6

  1. ncbi Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential
    Karen J Gregory
    Department of Pharmacology, Vanderbilt Program in Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232 0697, USA
    Neuropharmacology 60:66-81. 2011
    ..In the absence of a class C GPCR crystal structure, this approach has shown promise with respect to the interpretation of mutagenesis data and understanding structure-activity relationships of allosteric modulator pharmacophores...
  2. ncbi Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships
    Karen J Gregory
    Department of Pharmacology, Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Vanderbilt University Medical Center, Nashville, Tennessee 37232, USA
    Mol Pharmacol 82:860-75. 2012
    ..This model can be applied to PAM and NAM potency curves in combination with maximal fold-shift data to derive reliable estimates of modulator affinities...
  3. ncbi Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity
    Jerri M Rook
    Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232 0697, USA
    Biol Psychiatry 73:501-9. 2013
    ..This mechanism may be critical to maintaining normal activity-dependence of mGlu5 activation and achieving optimal in vivo effects...
  4. ncbi Allosteric modulation of metabotropic glutamate receptors
    Douglas J Sheffler
    Department of Pharmacology, Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    Adv Pharmacol 62:37-77. 2011
    ..Studies continue to validate the therapeutic utility of mGlu allosteric modulators as a potential therapeutic approach for a number of disorders including anxiety, schizophrenia, Parkinson's disease, and Fragile X syndrome...
  5. ncbi Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover
    Jason T Manka
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    Bioorg Med Chem Lett 22:6481-5. 2012
    ..These studies suggest that potent PAMs within topologically similar chemotypes can be developed to preferentially interact or not interact with the MPEP allosteric binding site...
  6. ncbi Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders
    Karen J Gregory
    Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    Prog Mol Biol Transl Sci 115:61-121. 2013
    ....