Karen J Gregory

Summary

Affiliation: Vanderbilt University
Country: USA

Publications

  1. pmc 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. pmc Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology
    Karen J Gregory
    Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232 0697, USA
    Mol Pharmacol 83:991-1006. 2013
  3. pmc 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
  4. pmc 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
  5. pmc 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
  6. pmc 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
  7. doi request reprint 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 Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee, USA Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia
    Prog Mol Biol Transl Sci 115:61-121. 2013

Collaborators

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

Detail Information

Publications7

  1. pmc 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. pmc Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology
    Karen J Gregory
    Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232 0697, USA
    Mol Pharmacol 83:991-1006. 2013
    ..Interestingly, we identified two point mutations in TMs 6 and 7 that, when mutated, engender a mode switch in the pharmacology of certain PAMs...
  3. pmc 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...
  4. pmc 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...
  5. pmc 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...
  6. pmc 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...
  7. doi request reprint 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 Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee, USA Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia
    Prog Mol Biol Transl Sci 115:61-121. 2013
    ....