Literature DB >> 21531137

Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype.

Anette Graven Sams1, Gitte Kobberøe Mikkelsen, Robbin M Brodbeck, Xiaosui Pu, Andreas Ritzén.   

Abstract

A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, and the underlying SAR is detailed.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21531137     DOI： 10.1016/j.bmcl.2011.03.103

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  10 in total

1.  Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation.

Authors:  Karen J Gregory; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2015-03-25       Impact factor: 4.436

Review 2.  Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Authors:  Shaun R Stauffer
Journal:  ACS Chem Neurosci       Date:  2011-06-27       Impact factor: 4.418

Review 3.  Drugs for allosteric sites on receptors.

Authors:  Cody J Wenthur; Patrick R Gentry; Thomas P Mathews; Craig W Lindsley
Journal:  Annu Rev Pharmacol Toxicol       Date:  2013-10-02       Impact factor: 13.820

4.  Drug Design Strategies for GPCR Allosteric Modulators.

Authors:  P Jeffrey Conn; Scott D Kuduk; Darío Doller
Journal:  Annu Rep Med Chem       Date:  2012       Impact factor: 1.059

5.  Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Authors:  Mark Turlington; Meredith J Noetzel; Aspen Chun; Ya Zhou; Rocco D Gogliotti; Elizabeth D Nguyen; Karen J Gregory; Paige N Vinson; Jerri M Rook; Kiran K Gogi; Zixiu Xiang; Thomas M Bridges; J Scott Daniels; Carrie Jones; Colleen M Niswender; Jens Meiler; P Jeffrey Conn; Craig W Lindsley; Shaun R Stauffer
Journal:  J Med Chem       Date:  2013-10-09       Impact factor: 7.446

6.  Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.

Authors:  Jason T Manka; Paige N Vinson; Karen J Gregory; Ya Zhou; Richard Williams; Kiran Gogi; Emily Days; Satya Jadhav; Elizabeth J Herman; Hilde Lavreysen; Claire Mackie; José M Bartolomé; Gregor J Macdonald; Thomas Steckler; J Scott Daniels; C David Weaver; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Shaun R Stauffer
Journal:  Bioorg Med Chem Lett       Date:  2012-08-24       Impact factor: 2.823

7.  Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.

Authors:  Karen J Gregory; Meredith J Noetzel; Jerri M Rook; Paige N Vinson; Shaun R Stauffer; Alice L Rodriguez; Kyle A Emmitte; Ya Zhou; Aspen C Chun; Andrew S Felts; Brian A Chauder; Craig W Lindsley; Colleen M Niswender; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2012-08-03       Impact factor: 4.436

8.  Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators.

Authors:  Karen J Gregory; Ranganadh Velagaleti; David M Thal; Ryan M Brady; Arthur Christopoulos; P Jeffrey Conn; David J Lapinsky
Journal:  ACS Chem Biol       Date:  2016-05-04       Impact factor: 5.100

9.  VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy.

Authors:  Hilary Highfield Nickols; Joannes P Yuh; Karen J Gregory; Ryan D Morrison; Brittney S Bates; Shaun R Stauffer; Kyle A Emmitte; Michael Bubser; Weimin Peng; Michael T Nedelcovych; Analisa Thompson; Xiaohui Lv; Zixiu Xiang; J Scott Daniels; Colleen M Niswender; Craig W Lindsley; Carrie K Jones; P Jeffrey Conn
Journal:  J Pharmacol Exp Ther       Date:  2015-10-26       Impact factor: 4.030

10.  Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.

Authors:  Kasper Harpsøe; Vignir Isberg; Benjamin G Tehan; Dahlia Weiss; Angela Arsova; Fiona H Marshall; Hans Bräuner-Osborne; David E Gloriam
Journal:  Sci Rep       Date:  2015-09-11       Impact factor: 4.379
  10 in total

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