Metabotropic glutamate receptor 3
Encyclopedia
Metabotropic glutamate receptor 3 is a protein
that in humans is encoded by the GRM3 gene
.
strategy.
with GRIP1
, PICK1
and PPM1A
.
Protein
Proteins are biochemical compounds consisting of one or more polypeptides typically folded into a globular or fibrous form, facilitating a biological function. A polypeptide is a single linear polymer chain of amino acids bonded together by peptide bonds between the carboxyl and amino groups of...
that in humans is encoded by the GRM3 gene
Gene
A gene is a molecular unit of heredity of a living organism. It is a name given to some stretches of DNA and RNA that code for a type of protein or for an RNA chain that has a function in the organism. Living beings depend on genes, as they specify all proteins and functional RNA chains...
.
Ligands
Though truly mGluR3 selective agents still await their discovery, mixed mGluR2/3 (group-II) ligands with selectivity over other mGluR-subtypes are known (2008). Low oral bioavailability is observed in some of them, but it can be met by applying a prodrugProdrug
A prodrug is a pharmacological substance administered in an inactive form. Once administered, the prodrug is metabolised in vivo into an active metabolite, a process termed bioactivation. The rationale behind the use of a prodrug is generally for absorption, distribution, metabolism, and...
strategy.
Agonists
- with a bicyclo[3.1.0]hexane skeleton
- MGS-0028
- LY404040
- LY379268
- LY354740EglumegadEglumegad is a research drug developed by Eli Lilly and Company, which is being investigated for its potential in the treatment of anxiety and drug addiction. It is a glutamate derived compound and its mode of action implies a novel mechanism....
; its (+)-C4α-methyl analog is a GluR2 agonist / GluR3 antagonist
- (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid
Antagonists
- CECXGCECXGCECXG is a research drug which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors , with reasonable selectivity for mGluR3...
- 38x selectivity for mGlu3 over mGlu2 - LY-341,495LY-341,495LY-341,495 is a research drug developed by the pharmaceutical company Eli Lilly, which acts as a potent and selective orthosteric antagonist for the group II metabotropic glutamate receptors ....
and its 1-fluoro analog: potent orthosteric antagonists - MGS-0039, HYDIA (both with bicyclo[3.1.0]hexane skeleton)
Allosteric modulators
- MNI-137: inhibitior
- compound 7p: non-competitive antagonist (presumably allosteric inhibitor)
Interactions
Metabotropic glutamate receptor 3 has been shown to interactProtein-protein interaction
Protein–protein interactions occur when two or more proteins bind together, often to carry out their biological function. Many of the most important molecular processes in the cell such as DNA replication are carried out by large molecular machines that are built from a large number of protein...
with GRIP1
GRIP1 (gene)
Glutamate receptor-interacting protein 1 is a protein that in humans is encoded by the GRIP1 gene.-Interactions:GRIP1 has been shown to interact with GRIA4, Metabotropic glutamate receptor 3, GRIK2, GRIK3, GRIPAP1, GRIA2 and GRIA3....
, PICK1
PICK1
PRKCA-binding protein is a protein that in humans is encoded by the PICK1 gene.-Interactions:PICK1 has been shown to interact with HER2/neu, ACCN2, Metabotropic glutamate receptor 7, BNC1, Metabotropic glutamate receptor 3, GRIA4, Dopamine transporter, GRIK1, GRIK2, GRIK3, GRIA2 and GRIA3.-Further...
and PPM1A
PPM1A
Protein phosphatase 1A is an enzyme that in humans is encoded by the PPM1A gene.-Interactions:PPM1A has been shown to interact with Metabotropic glutamate receptor 3....
.