Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders
出版年份 2014 全文链接
标题
Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders
作者
关键词
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出版物
NATURE REVIEWS DRUG DISCOVERY
Volume 13, Issue 9, Pages 692-708
出版商
Springer Nature
发表日期
2014-09-01
DOI
10.1038/nrd4308
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注意:仅列出部分参考文献,下载原文获取全部文献信息。- A Unique Industrial – Academic Collaboration Towards the Next Generation of Schizophrenia Therapeutics
- (2014) Gregor Macdonald et al. CURRENT TOPICS IN MEDICINAL CHEMISTRY
- Selective Actions of Novel Allosteric Modulators Reveal Functional Heteromers of Metabotropic Glutamate Receptors in the CNS
- (2014) S. Yin et al. JOURNAL OF NEUROSCIENCE
- Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain
- (2014) Andrew S. Doré et al. NATURE
- Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100
- (2014) Nellie E Byun et al. NEUROPSYCHOPHARMACOLOGY
- Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator
- (2014) H. Wu et al. SCIENCE
- Is There a Path Forward for mGlu2 Positive Allosteric Modulators for the Treatment of Schizophrenia?
- (2013) Corey R. Hopkins ACS Chemical Neuroscience
- Allosteric Modulators for the Treatment of Schizophrenia: Targeting Glutamatergic Networks
- (2013) Frank S. Menniti et al. CURRENT TOPICS IN MEDICINAL CHEMISTRY
- Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease
- (2013) Bruce J. Melancon et al. DRUG DISCOVERY TODAY
- mGlu5negative allosteric modulators: a patent review (2010 – 2012)
- (2013) Kyle A Emmitte EXPERT OPINION ON THERAPEUTIC PATENTS
- The Concept of Allosteric Interaction and Its Consequences for the Chemistry of the Brain
- (2013) Jean-Pierre Changeux JOURNAL OF BIOLOGICAL CHEMISTRY
- Discovery of (R)-(2-Fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-Hydroxypiperidin-1-yl)methanone (ML337), An mGlu3 Selective and CNS Penetrant Negative Allosteric Modulator (NAM)
- (2013) Cody J. Wenthur et al. JOURNAL OF MEDICINAL CHEMISTRY
- Synthesis and Pharmacological Profiling of Analogues of Benzyl Quinolone Carboxylic Acid (BQCA) as Allosteric Modulators of the M1 Muscarinic Receptor
- (2013) Shailesh N. Mistry et al. JOURNAL OF MEDICINAL CHEMISTRY
- Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning
- (2013) J. Xu et al. LEARNING & MEMORY
- Structure of class B GPCR corticotropin-releasing factor receptor 1
- (2013) Kaspar Hollenstein et al. NATURE
- Activation and allosteric modulation of a muscarinic acetylcholine receptor
- (2013) Andrew C. Kruse et al. NATURE
- Signalling bias in new drug discovery: detection, quantification and therapeutic impact
- (2013) Terry Kenakin et al. NATURE REVIEWS DRUG DISCOVERY
- Emerging paradigms in GPCR allostery: implications for drug discovery
- (2013) Denise Wootten et al. NATURE REVIEWS DRUG DISCOVERY
- Development of allosteric modulators of GPCRs for treatment of CNS disorders
- (2013) Hilary Highfield Nickols et al. NEUROBIOLOGY OF DISEASE
- Mechanism based neurotoxicity of mGlu5 positive allosteric modulators – Development challenges for a promising novel antipsychotic target
- (2013) Sophie Parmentier-Batteur et al. NEUROPHARMACOLOGY
- Assessment and Challenges of Ligand Docking into Comparative Models of G-Protein Coupled Receptors
- (2013) Elizabeth Dong Nguyen et al. PLoS One
- Chemical Modification of the M1 Agonist VU0364572 Reveals Molecular Switches in Pharmacology and a Bitopic Binding Mode
- (2012) Gregory J. Digby et al. ACS Chemical Neuroscience
- Structure-Function of the G Protein–Coupled Receptor Superfamily
- (2012) Vsevolod Katritch et al. Annual Review of Pharmacology and Toxicology
- Emerging opportunities for allosteric modulation of G-protein coupled receptors
- (2012) Ching-I. Anderson Wang et al. BIOCHEMICAL PHARMACOLOGY
- 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
- mGluR5 Negative Allosteric Modulators Overview: A Medicinal Chemistry Approach Towards a Series of Novel Therapeutic Agents
- (2012) Jean-Philippe Rocher et al. CURRENT TOPICS IN MEDICINAL CHEMISTRY
- Identification of Molecular Phenotypes and Biased Signaling Induced by Naturally Occurring Mutations of the Human Calcium-Sensing Receptor
- (2012) Katie Leach et al. ENDOCRINOLOGY
- Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature
- (2012) Craig W Lindsley et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- Allosteric Modulator ORG27569 Induces CB1 Cannabinoid Receptor High Affinity Agonist Binding State, Receptor Internalization, and GiProtein-independent ERK1/2 Kinase Activation
- (2012) Kwang H. Ahn et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Novel Allosteric Agonists of M1 Muscarinic Acetylcholine Receptors Induce Brain Region-Specific Responses That Correspond with Behavioral Effects in Animal Models
- (2012) G. J. Digby et al. JOURNAL OF NEUROSCIENCE
- Role of metabotropic glutamate receptors in persistent forms of hippocampal plasticity and learning
- (2012) Sreedeep Mukherjee et al. NEUROPHARMACOLOGY
- The mGlu5 positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat
- (2012) Francois Gastambide et al. NEUROPHARMACOLOGY
- Pharmacological profiling of native group II metabotropic glutamate receptors in primary cortical neuronal cultures using a FLIPR
- (2012) Helen Sanger et al. NEUROPHARMACOLOGY
- Synergy between l-DOPA and a novel positive allosteric modulator of metabotropic glutamate receptor 4: Implications for Parkinson's disease treatment and dyskinesia
- (2012) Khaled-Ezaheir Bennouar et al. NEUROPHARMACOLOGY
- Functional importance of GLP-1 receptor species and expression levels in cell lines
- (2012) Lotte Bjerre Knudsen et al. REGULATORY PEPTIDES
- Drugs for Allosteric Sites on Receptors
- (2011) Cody J. Wenthur et al. Annual Review of Pharmacology and Toxicology
- “Molecular Switches” on mGluR Allosteric Ligands That Modulate Modes of Pharmacology
- (2011) Michael R. Wood et al. BIOCHEMISTRY
- Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators
- (2011) L Lundström et al. BRITISH JOURNAL OF PHARMACOLOGY
- Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor
- (2011) Anna E. Davey et al. ENDOCRINOLOGY
- Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery
- (2011) Bruce J. Melancon et al. JOURNAL OF MEDICINAL CHEMISTRY
- Selective Remediation of Reversal Learning Deficits in the Neurodevelopmental MAM Model of Schizophrenia by a Novel mGlu5 Positive Allosteric Modulator
- (2011) Francois Gastambide et al. NEUROPSYCHOPHARMACOLOGY
- Allosteric Modulation of Family C G-Protein-Coupled Receptors: from Molecular Insights to Therapeutic Perspectives
- (2011) S. Urwyler PHARMACOLOGICAL REVIEWS
- Dimers and beyond: The functional puzzles of class C GPCRs
- (2011) Julie Kniazeff et al. PHARMACOLOGY & THERAPEUTICS
- Allostery in GPCRs: ‘MWC’ revisited
- (2011) Meritxell Canals et al. TRENDS IN BIOCHEMICAL SCIENCES
- Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development
- (2011) Julia K. Archbold et al. TRENDS IN PHARMACOLOGICAL SCIENCES
- Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease
- (2010) Colleen M. Niswender et al. Annual Review of Pharmacology and Toxicology
- Exploring a role for heteromerization in GPCR signalling specificity
- (2010) Raphael Rozenfeld et al. BIOCHEMICAL JOURNAL
- Impact of species variability and ‘probe-dependence’ on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor
- (2010) S Suratman et al. BRITISH 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
- Chemical Switch of a Metabotropic Glutamate Receptor 2 Silent Allosteric Modulator into Dual Metabotropic Glutamate Receptor 2/3 Negative/Positive Allosteric Modulators
- (2010) Stephan Schann et al. JOURNAL OF MEDICINAL CHEMISTRY
- 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
- Effects of the Allosteric Antagonist 1-(4-Chlorophenyl)-3-[3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl]urea (PSNCBAM-1) on CB1 Receptor Modulation in the Cerebellum
- (2010) X. Wang et al. MOLECULAR PHARMACOLOGY
- Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor
- (2010) Michael P. Bokoch et al. NATURE
- Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential
- (2010) Karen J. Gregory et al. NEUROPHARMACOLOGY
- Differential effects of the mGluR5 positive allosteric modulator CDPPB in the cortex and striatum following repeated administration
- (2010) Sophie Parmentier-Batteur et al. NEUROPHARMACOLOGY
- Loss of Object Recognition Memory Produced by Extended Access to Methamphetamine Self-Administration is Reversed by Positive Allosteric Modulation of Metabotropic Glutamate Receptor 5
- (2010) Carmela M Reichel et al. NEUROPSYCHOPHARMACOLOGY
- Discovery and Characterization of Novel Subtype-Selective Allosteric Agonists for the Investigation of M1 Receptor Function in the Central Nervous System
- (2009) Evan P Lebois et al. ACS Chemical Neuroscience
- Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist
- (2009) Atsushi Satoh et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M1 positive allosteric modulators
- (2009) Feng V. Yang et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- The role of dimerisation in the cellular trafficking of G-protein-coupled receptors
- (2009) Graeme Milligan CURRENT OPINION IN PHARMACOLOGY
- Discovery of Molecular Switches That Modulate Modes of Metabotropic Glutamate Receptor Subtype 5 (mGlu5) Pharmacology in Vitro and in Vivo within a Series of Functionalized, Regioisomeric 2- and 5-(Phenylethynyl)pyrimidines
- (2009) Sameer Sharma et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-TrifluoromethoxyN-Benzyl Isatins
- (2009) Thomas M. Bridges et al. JOURNAL OF MEDICINAL CHEMISTRY
- A Selective Allosteric Potentiator of the M1 Muscarinic Acetylcholine Receptor Increases Activity of Medial Prefrontal Cortical Neurons and Restores Impairments in Reversal Learning
- (2009) J. K. Shirey et al. JOURNAL OF NEUROSCIENCE
- Context-Dependent Pharmacology Exhibited by Negative Allosteric Modulators of Metabotropic Glutamate Receptor 7
- (2009) C. M. Niswender et al. MOLECULAR PHARMACOLOGY
- Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties
- (2009) Katie Leach et al. NEUROPSYCHOPHARMACOLOGY
- mGluR5 Positive Allosteric Modulators Facilitate both Hippocampal LTP and LTD and Enhance Spatial Learning
- (2009) Jennifer E Ayala et al. NEUROPSYCHOPHARMACOLOGY
- Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation
- (2009) L. Ma et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Interaction of N-methyl-D-aspartate and group 5 metabotropic glutamate receptors on behavioral flexibility using a novel operant set-shift paradigm
- (2008) Justin M. Darrah et al. BEHAVIOURAL PHARMACOLOGY
- Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold
- (2008) Sameer Sharma et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Characterization of a CNS penetrant, selective M1muscarinic receptor agonist, 77-LH-28-1
- (2008) C J Langmead et al. BRITISH JOURNAL OF PHARMACOLOGY
- A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity
- (2008) Celine Valant et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Novel Selective Allosteric Activator of the M1 Muscarinic Acetylcholine Receptor Regulates Amyloid Processing and Produces Antipsychotic-Like Activity in Rats
- (2008) C. K. Jones et al. JOURNAL OF NEUROSCIENCE
- 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
- Centrally Active Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats
- (2008) A. E. Brady et al. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
- Mutagenic Mapping Suggests a Novel Binding Mode for Selective Agonists of M1 Muscarinic Acetylcholine Receptors
- (2008) G. Lebon et al. MOLECULAR PHARMACOLOGY
- Discovery, Characterization, and Antiparkinsonian Effect of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4
- (2008) C. M. Niswender et al. MOLECULAR PHARMACOLOGY
- Allosteric Ligands for the Corticotropin Releasing Factor Type 1 Receptor Modulate Conformational States Involved in Receptor Activation
- (2008) S. R. J. Hoare et al. MOLECULAR PHARMACOLOGY
- Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity
- (2008) J. E. Marlo et al. MOLECULAR PHARMACOLOGY
- Structural diversity of G protein-coupled receptors and significance for drug discovery
- (2008) Malin C. Lagerström et al. NATURE REVIEWS DRUG DISCOVERY
- Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
- (2008) P. Jeffrey Conn et al. NATURE REVIEWS DRUG DISCOVERY
- Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells
- (2008) Douglas J. Sheffler et al. NEUROPHARMACOLOGY
- Receptor activation involving positive allosteric modulation, unlike full agonism, does not result in GABAB receptor desensitization
- (2008) Tina Gjoni et al. NEUROPHARMACOLOGY
- Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract–piriform cortex synapse
- (2008) Paulianda J. Jones et al. NEUROPHARMACOLOGY
- Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia
- (2008) W. Y. Chan et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
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