Fragile X syndrome: a preclinical review on metabotropic glutamate receptor 5 (mGluR5) antagonists and drug development (Q38162720)

30 August 2017

Fragile X syndrome: a preclinical review on metabotropic glutamate receptor 5 (mGluR5) antagonists and drug development (English)

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30 August 2017

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Andreea S Pop

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30 August 2017

Baltazar Gomez-Mancilla

2

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30 August 2017

Giovanni Neri

3

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30 August 2017

Rob Willemsen

4

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30 August 2017

Fabrizio Gasparini

5

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30 August 2017

1 March 2014

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30 August 2017

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30 August 2017

231

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30 August 2017

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30 August 2017

1217-1226

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https://scigraph.springernature.com/pub.10.1007/s00213-013-3330-3

30 August 2017

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cites work

Nucleus basalis magnocellularis and hippocampus are the major sites of FMR-1 expression in the human fetal brain.

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The mGluR theory of fragile X mental retardation

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Open-label treatment trial of lithium to target the underlying defect in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Minocycline promotes dendritic spine maturation and improves behavioural performance in the fragile X mouse model

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The FMR1 gene and fragile X-associated tremor/ataxia syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Microarray identification of FMRP-associated brain mRNAs and altered mRNA translational profiles in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Complex effects of mGluR5 antagonism on sociability and stereotypic behaviors in mice: possible implications for the pharmacotherapy of autism spectrum disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Fragile X mice develop sensory hyperreactivity to auditory stimuli

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Synergistic effect of histone hyperacetylation and DNA demethylation in the reactivation of the FMR1 gene.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Acetylated histones are associated with FMR1 in normal but not fragile X-syndrome cells.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Fragile X mental retardation protein has a unique, evolutionarily conserved neuronal function not shared with FXR1P or FXR2P

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Highly conserved 3' UTR and expression pattern of FXR1 points to a divergent gene regulation of FXR1 and FMR1

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Cytoplasmic RNA-binding proteins and the control of complex brain function

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

FMRP stalls ribosomal translocation on mRNAs linked to synaptic function and autism

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Transport of fragile X mental retardation protein via granules in neurites of PC12 cells

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Rescue of behavioral phenotype and neuronal protrusion morphology in Fmr1 KO mice

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Generation and characterization of FMR1 knockout zebrafish

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The FMR-1 protein is cytoplasmic, most abundant in neurons and appears normal in carriers of a fragile X premutation

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Regulation of metabotropic glutamate receptor signaling, desensitization and endocytosis

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Mildly impaired water maze performance in male Fmr1 knockout mice.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Decreased expression of the GABAA receptor in fragile X syndrome.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Drosophila lacking dfmr1 activity show defects in circadian output and fail to maintain courtship interest

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Correction of fragile X syndrome in mice.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Decreased GABA(A) receptor expression in the seizure-prone fragile X mouse.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The fragile X mental retardation protein-RNP granules show an mGluR-dependent localization in the post-synaptic spines

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Chronic administration of AFQ056/Mavoglurant restores social behaviour in Fmr1 knockout mice

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Temporal requirements of the fragile X mental retardation protein in the regulation of synaptic structure

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

A reduced number of metabotropic glutamate subtype 5 receptors are associated with constitutive homer proteins in a mouse model of fragile X syndrome.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Excess phosphoinositide 3-kinase subunit synthesis and activity as a novel therapeutic target in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Ablation of Fmrp in adult neural stem cells disrupts hippocampus-dependent learning

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Tissue specific expression of FMR-1 provides evidence for a functional role in fragile X syndrome.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Analysis of neocortex in three males with the fragile X syndrome

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Altered mTOR signaling and enhanced CYFIP2 expression levels in subjects with fragile X syndrome

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Altered synaptic plasticity in a mouse model of fragile X mental retardation

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Dendritic spine structural anomalies in fragile-X mental retardation syndrome

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Abnormal dendritic spine characteristics in the temporal and visual cortices of patients with fragile-X syndrome: a quantitative examination.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Epigenetic modification of the FMR1 gene in fragile X syndrome is associated with differential response to the mGluR5 antagonist AFQ056.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Learning and memory deficits consequent to reduction of the fragile X mental retardation protein result from metabotropic glutamate receptor-mediated inhibition of cAMP signaling in Drosophila.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Altered mRNA transport, docking, and protein translation in neurons lacking fragile X mental retardation protein

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Cognitive dysfunction and prefrontal synaptic abnormalities in a mouse model of fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Interaction of the transcription factors USF1, USF2, and alpha -Pal/Nrf-1 with the FMR1 promoter. Implications for Fragile X mental retardation syndrome

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Species-dependent posttranscriptional regulation of NOS1 by FMRP in the developing cerebral cortex.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Potential therapeutic interventions for fragile X syndrome

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Perisynaptic location of metabotropic glutamate receptors mGluR1 and mGluR5 on dendrites and dendritic spines in the rat hippocampus

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Characterization of the full fragile X syndrome mutation in fetal gametes.

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

A PEDIGREE OF MENTAL DEFECT SHOWING SEX-LINKAGE.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Evidence for social anxiety and impaired social cognition in a mouse model of fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The generation of a conditional Fmr1 knock out mouse model to study Fmrp function in vivo.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Elevated glycogen synthase kinase-3 activity in Fragile X mice: key metabolic regulator with evidence for treatment potential.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Social approach in genetically engineered mouse lines relevant to autism

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

A distinct DNA-methylation boundary in the 5'- upstream sequence of the FMR1 promoter binds nuclear proteins and is lost in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Alterations in the auditory startle response in Fmr1 targeted mutant mouse models of fragile X syndrome.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Metabotropic receptor-dependent long-term depression persists in the absence of protein synthesis in the mouse model of fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Instability of a 550-base pair DNA segment and abnormal methylation in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The Drosophila fragile X gene negatively regulates neuronal elaboration and synaptic differentiation

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Fragile X mouse: strain effects of knockout phenotype and evidence suggesting deficient amygdala function.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

(Over)correction of FMR1 deficiency with YAC transgenics: behavioral and physical features

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Absence of expression of the FMR-1 gene in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Genetic-background modulation of core and variable autistic-like symptoms in Fmr1 knock-out mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Which comes first in fragile X syndrome, dendritic spine dysgenesis or defects in circuit plasticity?

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Neurodevelopmental effects of the FMR-1 full mutation in humans.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Enriched environment promotes behavioral and morphological recovery in a mouse model for the fragile X syndrome.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

mGluR5 negative allosteric modulators overview: a medicinal chemistry approach towards a series of novel therapeutic agents

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Metabotropic glutamate receptors and fragile x mental retardation protein: partners in translational regulation at the synapse

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Adult fragile X syndrome. Clinico-neuropathologic findings.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Psychometric study of the Aberrant Behavior Checklist in Fragile X Syndrome and implications for targeted treatment

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Adult fragile X syndrome: neuropsychology, brain anatomy, and metabolism.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Fragile X mental retardation protein regulates the levels of scaffold proteins and glutamate receptors in postsynaptic densities

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Epigenetic characterization of the FMR1 gene and aberrant neurodevelopment in human induced pluripotent stem cell models of fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Normal phenotype in two brothers with a full FMR1 mutation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Altered anxiety-related and social behaviors in the Fmr1 knockout mouse model of fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Modifying behavioral phenotypes in Fmr1KO mice: genetic background differences reveal autistic-like responses

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Testing the FMR1 promoter for mosaicism in DNA methylation among CpG sites, strands, and cells in FMR1-expressing males with fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Early continuous inhibition of group 1 mGlu signaling partially rescues dendritic spine abnormalities in the Fmr1 knockout mouse model for fragile X syndrome.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

DNA methylation represses FMR-1 transcription in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Differential epigenetic modifications in the FMR1 gene of the fragile X syndrome after reactivating pharmacological treatments.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Modest reactivation of the mutant FMR1 gene by valproic acid is accompanied by histone modifications but not DNA demethylation

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Epigenetic analysis reveals a euchromatic configuration in the FMR1 unmethylated full mutations.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The mGluR5 antagonist AFQ056 does not affect methylation and transcription of the mutant FMR1 gene in vitro

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Fragile X males with unmethylated, full mutation trinucleotide repeat expansions have elevated levels of FMR1 messenger RNA.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Elevated FMR1 mRNA in premutation carriers is due to increased transcription.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Group I metabotropic glutamate receptor antagonists alter select behaviors in a mouse model for fragile X syndrome.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Altered maturation of the primary somatosensory cortex in a mouse model of fragile X syndrome.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The psychiatric presentation of fragile x: evolution of the diagnosis and treatment of the psychiatric comorbidities of fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Expression of three zebrafish orthologs of human FMR1-related genes and their phylogenetic relationships.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Contribution of mGluR and Fmr1 functional pathways to neurite morphogenesis, craniofacial development and fragile X syndrome.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Population screening for fragile X

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Characterisation of Fmrp in zebrafish: evolutionary dynamics of the fmr1 gene

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Identification of a gene (FMR-1) containing a CGG repeat coincident with a breakpoint cluster region exhibiting length variation in fragile X syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The effect of an mGluR5 inhibitor on procedural memory and avoidance discrimination impairments in Fmr1 KO mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Activation of the extracellular signal-regulated kinase pathway contributes to the behavioral deficit of fragile x-syndrome.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Fragile X mental retardation protein is translated near synapses in response to neurotransmitter activation

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Association of FMRP with ribosomal precursor particles in the nucleolus

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Timing of the absence of FMR1 expression in full mutation chorionic villi.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Suppression of two major Fragile X Syndrome mouse model phenotypes by the mGluR5 antagonist MPEP.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Fragile X genotype characterized by an unstable region of DNA.

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

The fragile X syndrome protein FMRP associates with BC1 RNA and regulates the translation of specific mRNAs at synapses

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

A new function for the fragile X mental retardation protein in regulation of PSD-95 mRNA stability

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

A mouse model of the human Fragile X syndrome I304N mutation

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Drosophila fragile X-related gene regulates the MAP1B homolog Futsch to control synaptic structure and function

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Behavioral and neuroanatomical characterization of the Fmr1 knockout mouse

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

A heterogeneous set of FMR1 proteins is widely distributed in mouse tissues and is modulated in cell culture

21 January 2018

1 reference

https://api.crossref.org/works/10.1007%2FS00213-013-3330-3

Molecular characterization of a novel metabotropic glutamate receptor mGluR5 coupled to inositol phosphate/Ca2+ signal transduction

21 January 2018

1 reference

12 December 2020

The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate recepto

1 reference

12 December 2020

FXR1, an autosomal homolog of the fragile X mental retardation gene

1 reference

12 December 2020

Treatment with valproic acid ameliorates ADHD symptoms in fragile X syndrome boys

1 reference

12 December 2020

Fmr1 knockout mice: a model to study fragile X mental retardation. The Dutch-Belgian Fragile X Consortium

1 reference

12 December 2020

Fragile X mental retardation protein: nucleocytoplasmic shuttling and association with somatodendritic ribosomes

1 reference

12 December 2020

SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5

1 reference

12 December 2020

The fragile X mental retardation syndrome protein interacts with novel homologs FXR1 and FXR2

1 reference

12 December 2020

Recent progress in the discovery and development of negative allosteric modulators of mGluR5.

1 reference

12 December 2020

A marker X chromosome

1 reference

12 December 2020

10.1007/S00213-013-3330-3

Identifiers

DOI

1 reference

Dimensions Publication ID

30 August 2017

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1 reference