Genetic Reduction or Negative Modulation of mGlu7 Does Not Impact Anxiety and Fear Learning Phenotypes in a Mouse Model of MECP2 Duplication Syndrome.
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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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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
Sign Up to like & getrecommendations! 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