scholarly article | Q13442814 |
P6179 | Dimensions Publication ID | 1032059331 |
P356 | DOI | 10.1038/NRD4308 |
P2888 | exact match | https://scigraph.springernature.com/pub.10.1038/nrd4308 |
P932 | PMC publication ID | 4208620 |
P698 | PubMed publication ID | 25176435 |
P5875 | ResearchGate publication ID | 265212165 |
P50 | author | Jens Meiler | Q29315318 |
Colleen M. Niswender | Q67215380 | ||
Craig W. Lindsley | Q67215429 | ||
P. Jeffrey Conn | Q67215432 | ||
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"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology | Q37845809 | ||
Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development | Q37896837 | ||
Allostery in GPCRs: 'MWC' revisited. | Q37932797 | ||
Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature | Q38002888 | ||
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Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators | Q38649976 | ||
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 | Q38687186 | ||
Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode | Q39222571 | ||
Identification of molecular phenotypes and biased signaling induced by naturally occurring mutations of the human calcium-sensing receptor. | Q39314038 | ||
Functional importance of GLP-1 receptor species and expression levels in cell lines. | Q39411043 | ||
Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor. | Q39419158 | ||
A new approach to analyze cell surface protein complexes reveals specific heterodimeric metabotropic glutamate receptors. | Q39657918 | ||
Receptor activation involving positive allosteric modulation, unlike full agonism, does not result in GABAB receptor desensitization | Q39942670 | ||
A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. | Q39947679 | ||
A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties | Q40157034 | ||
Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. | Q40170457 | ||
Cyclic AMP-dependent and Epac-mediated activation of R-Ras by G protein-coupled receptors leads to phospholipase D stimulation | Q40271340 | ||
A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators | Q40374968 | ||
Adenosine A1 receptor-mediated modulation of dopamine D1 receptors in stably cotransfected fibroblast cells | Q41059064 | ||
Is there a path forward for mGlu(2) positive allosteric modulators for the treatment of schizophrenia? | Q41790775 | ||
Group I mGluR-induced epileptogenesis: distinct and overlapping roles of mGluR1 and mGluR5 and implications for antiepileptic drug design | Q42139378 | ||
Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes | Q42483396 | ||
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Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target | Q42713510 | ||
A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease | Q42717015 | ||
Synergy between L-DOPA and a novel positive allosteric modulator of metabotropic glutamate receptor 4: implications for Parkinson's disease treatment and dyskinesia | Q42719140 | ||
Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects | Q42726130 | ||
Discovery of an ectopic activation site on the M(1) muscarinic receptor | Q42815075 | ||
Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning | Q43082537 | ||
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 | Q43292922 | ||
Chemical induction of mGluR5- and protein synthesis--dependent long-term depression in hippocampal area CA1. | Q43657512 | ||
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Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor | Q44267726 | ||
The mGluR theory of fragile X mental retardation | Q29615060 | ||
Can the pharmaceutical industry reduce attrition rates? | Q29616077 | ||
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A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors | Q30406728 | ||
Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100 | Q30410518 | ||
N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement. | Q30427199 | ||
Allosteric modulation of metabotropic glutamate receptors | Q30448534 | ||
The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease. | Q30458705 | ||
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 | Q30472643 | ||
Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system | Q30474039 | ||
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation | Q30489795 | ||
Loss of object recognition memory produced by extended access to methamphetamine self-administration is reversed by positive allosteric modulation of metabotropic glutamate receptor 5 | Q30498430 | ||
Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties | Q30498538 | ||
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity | Q30535764 | ||
Structure-function of the G protein-coupled receptor superfamily | Q30576993 | ||
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. | Q33268568 | ||
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission | Q33308569 | ||
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Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators | Q33755292 | ||
mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning | Q33908562 | ||
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A new benzodiazepine pharmacology. | Q34106026 | ||
Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity | Q34123595 | ||
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. | Q34222874 | ||
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Development of allosteric modulators of GPCRs for treatment of CNS disorders | Q34373958 | ||
A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators | Q34518807 | ||
G protein-coupled receptor allosterism and complexing | Q34523552 | ||
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Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor. | Q34672123 | ||
ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activiti | Q34815750 | ||
The use of constitutively active GPCRs in drug discovery and functional genomics | Q34981350 | ||
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. | Q35688485 | ||
Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator | Q35760205 | ||
Allosteric modulators: the new generation of receptor antagonist | Q35860365 | ||
Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activation | Q35874442 | ||
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery | Q35952381 | ||
Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models | Q36099440 | ||
Functional and pharmacological characteristics of metabotropic glutamate receptors 2/4 heterodimers | Q36174739 | ||
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships | Q36335613 | ||
A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling | Q36717066 | ||
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 | Q36776760 | ||
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. | Q36880915 | ||
The prevalence, maintenance, and relevance of G protein-coupled receptor oligomerization | Q36935273 | ||
Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. | Q36959071 | ||
Calcium sensing receptor activators: calcimimetics | Q37066049 | ||
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl- d -aspartate receptor activity | Q37089832 | ||
Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract-piriform cortex synapse. | Q37101834 | ||
Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors | Q37199099 | ||
Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks | Q37220392 | ||
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders | Q37360436 | ||
Allosteric modulators of GABA(B) receptors: mechanism of action and therapeutic perspective. | Q37420482 | ||
The role of dimerisation in the cellular trafficking of G-protein-coupled receptors | Q37619942 | ||
Metabotropic glutamate receptors: physiology, pharmacology, and disease | Q37670222 | ||
G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives | Q37680849 | ||
Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential | Q37773480 | ||
P433 | issue | 9 | |
P407 | language of work or name | English | Q1860 |
P921 | main subject | G protein-coupled receptor | Q38173 |
P304 | page(s) | 692-708 | |
P577 | publication date | 2014-09-01 | |
P1433 | published in | Nature Reviews Drug Discovery | Q45998 |
P1476 | title | Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders | |
P478 | volume | 13 |
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Q90576739 | Challenges in the Discovery and Optimization of mGlu2/4 Heterodimer Positive Allosteric Modulators |
Q38876214 | Cinnabarinic acid and xanthurenic acid: Two kynurenine metabolites that interact with metabotropic glutamate receptors. |
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Q37167965 | Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators |
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Q50872293 | Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies. |
Q89394623 | Crystal structure of the human angiotensin II type 2 receptor bound to an angiotensin II analog |
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Q38436762 | Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition |
Q38437959 | Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core |
Q42271745 | Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). |
Q47887304 | Discovery of 2-Piperidinyl Phenyl Benzamides and Trisubstituted Pyrimidines as Positive Allosteric Modulators of the Prostaglandin Receptor EP2. |
Q42145142 | Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy |
Q36050350 | Discovery of Small-Molecule Modulators of the Human Y4 Receptor |
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Q46417915 | Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia |
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Q26739930 | Diverse modes of NMDA receptor positive allosteric modulation: Mechanisms and consequences |
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Q92949088 | Evaluation of Synthetic Cytochrome P450-Mimetic Metalloporphyrins To Facilitate "Biomimetic" Biotransformation of a Series of mGlu5 Allosteric Ligands |
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Q35671393 | From G Protein-coupled Receptor Structure Resolution to Rational Drug Design. |
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Q38878129 | Guidelines for the Synthesis of Small-Molecule Irreversible Probes Targeting G Protein-Coupled Receptors. |
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Q26773431 | Neurobiological Insights from mGlu Receptor Allosteric Modulation |
Q37140411 | New paradigms in GPCR drug discovery. |
Q88337997 | Niclosamide is a Negative Allosteric Modulator of Group I Metabotropic Glutamate Receptors: Implications for Neuropathic Pain |
Q38882060 | Nociception modulation by supraspinal group III metabotropic glutamate receptors |
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Q90679977 | Oligomeric Receptor Complexes and Their Allosteric Receptor-Receptor Interactions in the Plasma Membrane Represent a New Biological Principle for Integration of Signals in the CNS |
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Q48354605 | Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior. |
Q48001582 | Positive allosteric modulation of M1 and M4 muscarinic receptors as potential therapeutic treatments for schizophrenia |
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