Proteins > Metabotropic glutamate receptor 6
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Metabotropic glutamate receptor 6
A metabotropic glutamate receptor 6 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O15303]
Synonyms
mGluR6
Research
Bioassay Publications (10)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (30.00) | 18.2507 |
| 2000's | 3 (30.00) | 29.6817 |
| 2010's | 4 (40.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (31)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 2-amino-4-phosphonobutyric acid | Homo sapiens (human) | EC50 | 0.2800 | 1 | 1 |
| aspartic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| kainic acid | Homo sapiens (human) | EC50 | 299.0000 | 1 | 1 |
| d-glutamate | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| glutamic acid | Homo sapiens (human) | EC50 | 98.3000 | 3 | 3 |
| d-aspartic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| L-2-aminoadipic acid | Homo sapiens (human) | EC50 | 140.0000 | 1 | 1 |
| alpha-aminopimelic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Homo sapiens (human) | EC50 | 82.0000 | 1 | 1 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | EC50 | 220.0000 | 1 | 1 |
| alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| 2-amino-4-phosphonobutyric acid | Homo sapiens (human) | EC50 | 1.1517 | 3 | 3 |
| eglumetad | Homo sapiens (human) | EC50 | 3.1750 | 2 | 2 |
| ampa, (r)-isomer | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| 1-aminocyclopentane-1,3,4-tricarboxylic acid | Homo sapiens (human) | EC50 | 11.0000 | 1 | 1 |
| ly 379268 | Homo sapiens (human) | EC50 | 50.2005 | 2 | 2 |
| 3,4-dicarboxyphenylglycine | Homo sapiens (human) | EC50 | 3.2000 | 1 | 1 |
| lsp4-2022 | Homo sapiens (human) | EC50 | 4.2000 | 1 | 1 |
Drugs with Other Measurements
Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Structural Basis for ( S)-3,4-Dicarboxyphenylglycine (DCPG) As a Potent and Subtype Selective Agonist of the mGluJournal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| glutamate receptor activity | molecular function | Combining with glutamate and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:ai, GOC:signaling] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| adenylate cyclase inhibiting G protein-coupled glutamate receptor activity | molecular function | Combining with glutamate and transmitting the signal across the membrane by activating the alpha-subunit of an associated heterotrimeric G-protein complex to inhibit downstream adenylate cyclase activity. [GOC:bf, GOC:dph] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| Golgi membrane | cellular component | The lipid bilayer surrounding any of the compartments of the Golgi apparatus. [GOC:mah] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| new growing cell tip | cellular component | A cell tip that was newly formed at the last cell division, and that has started to grow after the cell has activated bipolar cell growth (i.e. in which new end take-off, NETO, has taken place). New end take-off is when monopolar cells initiate bipolar growth. [GOC:expert_jd, GOC:mah, PMID:19431238] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|
| adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by glutamate binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| G protein-coupled glutamate receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by glutamate binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, GOC:signaling, PMID:9131252] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
| locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
| detection of visible light | biological process | The series of events in which a visible light stimulus is received by a cell and converted into a molecular signal. A visible light stimulus is electromagnetic radiation that can be perceived visually by an organism; for organisms lacking a visual system, this can be defined as light with a wavelength within the range 380 to 780 nm. [GOC:go_curators, ISBN:0198506732] |
| detection of light stimulus involved in visual perception | biological process | The series of events involved in visual perception in which a light stimulus is received and converted into a molecular signal. [GOC:ai, GOC:dos] |
| retina development in camera-type eye | biological process | The process whose specific outcome is the progression of the retina over time, from its formation to the mature structure. The retina is the innermost layer or coating at the back of the eyeball, which is sensitive to light and in which the optic nerve terminates. [GOC:bf, GOC:dph, ISBN:0815340729] |
| positive regulation of calcium ion import across plasma membrane | biological process | Any process that activates or increases the frequency, rate or extent of calcium ion import across plasma membrane. [GO_REF:0000058, GOC:bhm, GOC:TermGenie, PMID:17640527] |
| regulation of synaptic transmission, glutamatergic | biological process | Any process that modulates the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |