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   Articles with "mglu7" as a keyword



Profiling the Impact of mGlu7/Elfn1 Protein Interactions on the Pharmacology of mGlu7 Allosteric Modulators

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recommendations! Published in 2025 at "ACS Chemical Neuroscience"

DOI: 10.1021/acschemneuro.5c00174

Abstract: The group III metabotropic glutamate receptors (mGlu receptors) are predominantly expressed presynaptically throughout the central nervous system (CNS) where they regulate the release of glutamate and GABA. These receptors have recently been shown to be… read more here.

Keywords: allosteric modulators; mglu7; profiling impact; pharmacology ... See more keywords

Genetic Reduction or Negative Modulation of mGlu7 Does Not Impact Anxiety and Fear Learning Phenotypes in a Mouse Model of MECP2 Duplication Syndrome.

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recommendations! Published in 2018 at "ACS chemical neuroscience"

DOI: 10.1021/acschemneuro.7b00414

Abstract: Rett syndrome and MECP2 Duplication syndrome are neurodevelopmental disorders attributed to loss-of-function mutations in, or duplication of, the gene encoding methyl-CpG-binding protein 2 (MeCP2), respectively. We recently reported decreased expression and function of the metabotropic… read more here.

Keywords: mecp2 duplication; duplication; mglu7; duplication syndrome ... See more keywords

VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.

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recommendations! Published in 2017 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.7b00429

Abstract: Herein, we report the structure-activity relationships within a series of mGlu7 NAMs based on an N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration (Kp 1.9-5.8 and Kp,uu 0.4-1.4). Analogues in this series displayed steep SAR. Of these,… read more here.

Keywords: vu6010608 novel; trifluoromethoxy phenyl; mglu7; triazol trifluoromethoxy ... See more keywords

mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome

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recommendations! Published in 2017 at "Science Translational Medicine"

DOI: 10.1126/scitranslmed.aai7459

Abstract: mGlu7 positive allosteric modulation rescues long-term potentiation, learning, and memory phenotypes and prevents apneas in a mouse model of Rett syndrome. A positive approach to Rett syndrome Rett syndrome is an untreatable neurodevelopmental disorder. Gogliotti… read more here.

Keywords: mglu7; rett syndrome; model rett; mouse model ... See more keywords

Nedd4 E3 ligase and beta-arrestins regulate ubiquitination, trafficking, and stability of the mGlu7 receptor

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recommendations! Published in 2019 at "eLife"

DOI: 10.7554/elife.44502

Abstract: The metabotropic glutamate receptor 7 (mGlu7) is a class C G protein-coupled receptor that modulates excitatory neurotransmitter release at the presynaptic active zone. Although post-translational modification of cellular proteins with ubiquitin is a key molecular… read more here.

Keywords: regulate ubiquitination; arrestins regulate; receptor; mglu7 ... See more keywords