Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0U5DU)
Name
Glutamate receptor mGLU8 (mGluR8)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Metabotropic glutamate receptor 8; Group III metabotropic glutamate receptor 8; GRM8; Glutamate receptor mGLU8; MGLUR8; MGluR8a; mGluR8
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled glutamate receptor (GPCR-C)
Organism
Homo sapiens (Human)
Gene Name GRM8 Gene ID
2918
UniProt ID GRM8_HUMAN (click to find more protein-related data of this DBT)
TTD ID T77548 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGER
GVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFV
QALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTA
PELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISR
EIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQS
GHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFA
EFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMH
KDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITN
KSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCER
CEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTF
VIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMC
FSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPH
IIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEA
KPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYI
IIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTY
ISYSNHSI
Function
Receptor for glutamate. The activity of this receptor is mediated by a g-protein that inhibits adenylate cyclase activity.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Glutamic acid hydrochloride Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Acidulant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 5.7 nM (estimated based on the structural similarity with CHEMBL575060 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRM8_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 3400 nM (estimated based on the structural similarity with CHEMBL575060 ) [2]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID GRM8_RAT
          DIG Name: Monosodium glutamate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent; Flavoring agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 22 nM (estimated based on the structural similarity with CHEMBL575060 ) [3]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Mus musculus (Mouse)
                   UniProt ID GRM8_MOUSE
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 8000 nM (estimated based on the structural similarity with CHEMBL575060 ) [4]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID GRM8_RAT
References
1 (2S,1'S,2'R,3'R)-2(2'-Carboxy-3'-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors. Bioorg Med Chem Lett. 2005 Jan 17; 15(2):349-51.
2 Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines. Bioorg Med Chem. 2007 May 1; 15(9):3161-70.
3 Metabotropic glutamate receptors: novel targets for drug development. J Med Chem. 1995 Apr 28; 38(9):1417-26.
4 New probes of the agonist binding site of metabotropic glutamate receptors. Bioorg Med Chem Lett. 2001 Jun 18; 11(12):1569-72.

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