mGluR5: Exploration of Orthosteric and Allosteric Ligand Binding Pockets and Their Applications to Drug Discovery

Allosteric Modulators for the Treatment of Schizophrenia: Targeting Glutamatergic Networks

(2013) Frank S. Menniti et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

mGlu5negative allosteric modulators: a patent review (2010 – 2012)

(2013) Kyle A Emmitte   EXPERT OPINION ON THERAPEUTIC PATENTS

Glutamate Acts as a Partial Inverse Agonist to Metabotropic Glutamate Receptor with a Single Amino Acid Mutation in the Transmembrane Domain

(2013) Masataka Yanagawa et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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)

(2013) Mark Turlington et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of class B GPCR corticotropin-releasing factor receptor 1

(2013) Kaspar Hollenstein et al.   NATURE

Structure of the human glucagon class B G-protein-coupled receptor

(2013) Fai Yiu Siu et al.   NATURE

Development of allosteric modulators of GPCRs for treatment of CNS disorders

(2013) Hilary Highfield Nickols et al.   NEUROBIOLOGY OF DISEASE

Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors

(2013) E. Doumazane et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Unique Signaling Profiles of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Determine Differences in In Vivo Activity

(2012) Jerri M. Rook et al.   BIOLOGICAL PSYCHIATRY

Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold

(2012) Alice L. Rodriguez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Glutamate Receptors as Therapeutic Targets for Parkinsons Disease

(2012) Kari Johnson et al.   CNS & Neurological Disorders-Drug Targets

A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential

(2012) Cyril Goudet et al.   FASEB JOURNAL

Distinct roles of metabotropic glutamate receptor dimerization in agonist activation and G-protein coupling

(2012) D. El Moustaine et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Sequential Inter- and Intrasubunit Rearrangements During Activation of Dimeric Metabotropic Glutamate Receptor 1

(2012) V. Hlavackova et al.   Science Signaling

“Molecular Switches” on mGluR Allosteric Ligands That Modulate Modes of Pharmacology

(2011) Michael R. Wood et al.   BIOCHEMISTRY

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

(2011) Tony Warne et al.   NATURE

Dimers and beyond: The functional puzzles of class C GPCRs

(2011) Julie Kniazeff et al.   PHARMACOLOGY & THERAPEUTICS

Discovery of a Novel Chemical Class of mGlu5 Allosteric Ligands with Distinct Modes of Pharmacology

(2010) Alexis S. Hammond et al.   ACS Chemical Neuroscience

Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease

(2010) Colleen M. Niswender et al.   Annual Review of Pharmacology and Toxicology

Group 5 metabotropic glutamate receptors: Role in modulating cortical activity and relevance to cognition

(2010) Houman Homayoun et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

A new approach to analyze cell surface protein complexes reveals specific heterodimeric metabotropic glutamate receptors

(2010) Etienne Doumazane et al.   FASEB JOURNAL

Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity

(2010) A. L. Rodriguez et al.   MOLECULAR PHARMACOLOGY

Exploration of structure-based drug design opportunities for mGluRs

(2010) Sid Topiol et al.   NEUROPHARMACOLOGY

The complexity of their activation mechanism opens new possibilities for the modulation of mGlu and GABAB class C G protein-coupled receptors

(2010) Philippe Rondard et al.   NEUROPHARMACOLOGY

Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential

(2010) Karen J. Gregory et al.   NEUROPHARMACOLOGY

Mechanism-based approaches to treating fragile X

(2010) Gül Dölen et al.   PHARMACOLOGY & THERAPEUTICS

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator

(2009) Andreas Ritzén et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular basis for amino acid sensing by family C G-protein-coupled receptors

(2009) P Wellendorph et al.   BRITISH JOURNAL OF PHARMACOLOGY

A pilot open label, single dose trial of fenobam in adults with fragile X syndrome

(2009) E Berry-Kravis et al.   JOURNAL OF MEDICAL GENETICS

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum et al.   NATURE

Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one

(2009) Junko Fukuda et al.   NEUROPHARMACOLOGY

Fragile X syndrome

(2008) Kathryn B Garber et al.   EUROPEAN JOURNAL OF HUMAN GENETICS

ADX47273 [S-(4-Fluoro-phenyl)- -methanone]: A Novel Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulator with Preclinical Antipsychotic-Like and Procognitive Activities

(2008) F. Liu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Structure of a β1-adrenergic G-protein-coupled receptor

(2008) Tony Warne et al.   NATURE

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

(2008) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

(2008) P. Jeffrey Conn et al.   TRENDS IN PHARMACOLOGICAL SCIENCES