Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0NH3U)
Name
Glutamate receptor mGLU4 (mGluR4)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Metabotropic glutamate receptor 4; GPRC1D; Group III metabotropic glutamate receptor 4; mGluR4
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled glutamate receptor (GPCR-C)
Organism
Homo sapiens (Human)
Gene Name GRM4 Gene ID
2914
UniProt ID GRM4_HUMAN (click to find more protein-related data of this DBT)
TTD ID T99402 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MPGKRGLGWWWARLPLCLLLSLYGPWMPSSLGKPKGHPHMNSIRIDGDITLGGLFPVHGR
GSEGKPCGELKKEKGIHRLEAMLFALDRINNDPDLLPNITLGARILDTCSRDTHALEQSL
TFVQALIEKDGTEVRCGSGGPPIITKPERVVGVIGASGSSVSIMVANILRLFKIPQISYA
STAPDLSDNSRYDFFSRVVPSDTYQAQAMVDIVRALKWNYVSTVASEGSYGESGVEAFIQ
KSREDGGVCIAQSVKIPREPKAGEFDKIIRRLLETSNARAVIIFANEDDIRRVLEAARRA
NQTGHFFWMGSDSWGSKIAPVLHLEEVAEGAVTILPKRMSVRGFDRYFSSRTLDNNRRNI
WFAEFWEDNFHCKLSRHALKKGSHVKKCTNRERIGQDSAYEQEGKVQFVIDAVYAMGHAL
HAMHRDLCPGRVGLCPRMDPVDGTQLLKYIRNVNFSGIAGNPVTFNENGDAPGRYDIYQY
QLRNDSAEYKVIGSWTDHLHLRIERMHWPGSGQQLPRSICSLPCQPGERKKTVKGMPCCW
HCEPCTGYQYQVDRYTCKTCPYDMRPTENRTGCRPIPIIKLEWGSPWAVLPLFLAVVGIA
ATLFVVITFVRYNDTPIVKASGRELSYVLLAGIFLCYATTFLMIAEPDLGTCSLRRIFLG
LGMSISYAALLTKTNRIYRIFEQGKRSVSAPRFISPASQLAITFSLISLQLLGICVWFVV
DPSHSVVDFQDQRTLDPRFARGVLKCDISDLSLICLLGYSMLLMVTCTVYAIKTRGVPET
FNEAKPIGFTMYTTCIVWLAFIPIFFGTSQSADKLYIQTTTLTVSVSLSASVSLGMLYMP
KVYIILFHPEQNVPKRKRSLKAVVTAATMSNKFTQKGNFRPNGEAKSELCENLEAPALAT
KQTYVTYTNHAI
Function
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling inhibits adenylate cyclase activity. G-protein coupled receptor for glutamate.
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 for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 1400 nM (estimated based on the structural similarity with CHEMBL575060 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRM4_HUMAN
          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 = 3200 nM (estimated based on the structural similarity with CHEMBL575060 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRM4_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 2880 nM (estimated based on the structural similarity with CHEMBL575060 ) [3]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID GRM4_RAT
References
1 Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands. Bioorg Med Chem. 2009 Jan 1; 17(1):242-50.
2 A highly selective agonist for the metabotropic glutamate receptor mGluR2. Med Chem Comm. (2011) 2:1120-1124.
3 -amino--fluorocyclopropanecarboxylic acids as a new tool for drug development: synthesis of glutamic acid analogs and agonist activity towards metabotropic glutamate receptor 4. Bioorg Med Chem. 2012 Aug 1; 20(15):4716-26.

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