Identification of Allosteric Modulators of Metabotropic Glutamate 7 Receptor Using Proteochemometric Modeling [PDF]
Journal of Chemical Information and Modeling, 2017 Proteochemometric modeling (PCM) is a computational approach that can be considered an extension of quantitative structure-activity relationship (QSAR) modeling, where a single model incorporates information for a family of targets and all the associated ligands instead of modeling activity versus one target.
Gary Tresadern +5 more
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Analgesia induced by the epigenetic drug, L-acetylcarnitine, outlasts the end of treatment in mouse models of chronic inflammatory and neuropathic pain [PDF]
, 2017 Background: L-acetylcarnitine, a drug marketed for the treatment of chronic pain, causes analgesia by epigenetically up-regulating type-2 metabotropic glutamate (mGlu2) receptors in the spinal cord.
Battaglia, Giuseppe +10 more
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Metabotropic glutamate receptor 2/3 (mGluR2/3) activation suppresses TRPV1 sensitization in mouse, but not human sensory neurons [PDF]
, 2018 The use of human tissue to validate putative analgesic targets identified in rodents is a promising strategy for improving the historically poor translational record of preclinical pain research.
Baranger, David A.A. +5 more
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Sequences within the C terminus of the metabotropic glutamate receptor 5 (mGluR5) are responsible for inner nuclear membrane localization [PDF]
, 2017 Traditionally, G-protein-coupled receptors (GPCR) are thought to be located on the cell surface where they transmit extracellular signals to the cytoplasm.
Harmon, Steven K. +4 more
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Incentive learning underlying cocaine relapse requires mGluR5 receptors located on dopamine D1 receptor-expressing neurons [PDF]
, 2010 Understanding the psychobiological basis of relapse remains a challenge in developing therapies for drug addiction. Relapse in cocaine addiction often occurs following exposure to environmental stimuli previously associated with drug taking.
Bilbao, Ainhoa +11 more
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The prion protein regulates glutamate-mediated Ca2+ entry and mitochondrial Ca2+ accumulation in neurons [PDF]
, 2017 The cellular prion protein (PrPC) whose conformational misfolding leads to the production of deadly prions, has a still-unclarified cellular function despite decades of intensive research.
Bertoli, Alessandro +8 more
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Hippocampal neuronal cells that accumulate α-synuclein fragments are more vulnerable to Aβ oligomer toxicity via mGluR5--implications for dementia with Lewy bodies. [PDF]
, 2014 BackgroundIn dementia with Lewy bodies (DLB) abnormal interactions between α-synuclein (α-syn) and beta amyloid (Aβ) result in selective degeneration of neurons in the neocortex, limbic system and striatum.
Cartier, Anna +9 more
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Metabotropic Glutamate Receptors 7 within the Nucleus Accumbens are Involved in Relief Learning in Rats [PDF]
Current Neuropharmacology, 2016 Relief learning is an appetitive association of a formally neutral cue with relief induced by the offset of an aversive stimulus. Since the nucleus accumbens mediates relief learning and accumbal metabotropic glutamate receptors 7 (mGluR7) modulate appetitive-like processes, we hypothesized that accumbal mGluR7 may be involved in the modulation of ...
Evelyn Kahl, Markus Fendt
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Reduction in Phencyclidine Induced Sensorimotor Gating Deficits in the Rat Following Increased System Xc − Activity in the Medial Prefrontal Cortex [PDF]
, 2013 Rationale: Aspects of schizophrenia, including deficits in sensorimotor gating, have been linked to glutamate dysfunction and/or oxidative stress in the prefrontal cortex. System xc −, a cystine–glutamate antiporter, is a poorly understood mechanism that
A Araque +81 more
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The actin‐binding protein Filamin‐A interacts with the metabotropic glutamate receptor type 7 [PDF]
FEBS Letters, 2002 A yeast two‐hybrid screen identified Filamin‐A as a binding partner of the metabotropic glutamate receptor type 7b (mGluR7b) splice variant. In addition, Filamin‐A interacted with mGluR4a, mGluR5a, mGluR5b, mGluR7a and mGluR8a. Domain mapping revealed that alternative splicing of mGluR4, mGluR7 and mGluR8 C‐termini regulated the interaction.
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