Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

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Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders is …
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scholarly articleQ13442814

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P6179Dimensions Publication ID1032059331
P356DOI10.1038/NRD4308
P2888exact matchhttps://scigraph.springernature.com/pub.10.1038/nrd4308
P932PMC publication ID4208620
P698PubMed publication ID25176435
P5875ResearchGate publication ID265212165

P50authorJens MeilerQ29315318
Colleen M. NiswenderQ67215380
Craig W. LindsleyQ67215429
P. Jeffrey ConnQ67215432
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Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.Q39419158
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Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic targetQ42713510
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Allosteric modulation of metabotropic glutamate receptorsQ30448534
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 activityQ30472643
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Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiationQ30489795
Loss of object recognition memory produced by extended access to methamphetamine self-administration is reversed by positive allosteric modulation of metabotropic glutamate receptor 5Q30498430
Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic propertiesQ30498538
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activityQ30535764
Structure-function of the G protein-coupled receptor superfamilyQ30576993
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.Q33268568
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmissionQ33308569
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mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learningQ33908562
Interaction of N-methyl-D-aspartate and group 5 metabotropic glutamate receptors on behavioral flexibility using a novel operant set-shift paradigmQ34021713
The angiotensin II AT2 receptor is an AT1 receptor antagonist.Q34086986
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 activityQ34123595
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.Q34222874
Pharmacological profiling of native group II metabotropic glutamate receptors in primary cortical neuronal cultures using a FLIPR.Q34278605
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Development of allosteric modulators of GPCRs for treatment of CNS disordersQ34373958
A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulatorsQ34518807
G protein-coupled receptor allosterism and complexingQ34523552
Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptorsQ34608007
Exploring a role for heteromerization in GPCR signalling specificityQ34660378
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 activitiQ34815750
The use of constitutively active GPCRs in drug discovery and functional genomicsQ34981350
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 modulatorQ35760205
Allosteric modulators: the new generation of receptor antagonistQ35860365
Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activationQ35874442
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discoveryQ35952381
Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal modelsQ36099440
Functional and pharmacological characteristics of metabotropic glutamate receptors 2/4 heterodimersQ36174739
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationshipsQ36335613
A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signalingQ36717066
Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacologyQ36776760
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.Q36880915
The prevalence, maintenance, and relevance of G protein-coupled receptor oligomerizationQ36935273
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: calcimimeticsQ37066049
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl- d -aspartate receptor activityQ37089832
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 receptorsQ37199099
Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networksQ37220392
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disordersQ37360436
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 receptorsQ37619942
Metabotropic glutamate receptors: physiology, pharmacology, and diseaseQ37670222
G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectivesQ37680849
Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potentialQ37773480
P433issue9
P407language of work or nameEnglishQ1860
P921main subjectG protein-coupled receptorQ38173
P304page(s)692-708
P577publication date2014-09-01
P1433published inNature Reviews Drug DiscoveryQ45998
P1476titleOpportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders
P478volume13

Reverse relations

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