General Information of Drug Therapeutic Target (DTT) (ID: TT0I76D)

DTT Name Metabotropic glutamate receptor 7 (mGluR7)
Synonyms mGluR7; GPRC1G
Gene Name GRM7
DTT Type
Literature-reported target
[1]
BioChemical Class
GPCR glutamate
UniProt ID
GRM7_HUMAN
TTD ID
T61243
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVQLRKLLRVLTLMKFPCCVLEVLLCALAAAARGQEMYAPHSIRIEGDVTLGGLFPVHAK
GPSGVPCGDIKRENGIHRLEAMLYALDQINSDPNLLPNVTLGARILDTCSRDTYALEQSL
TFVQALIQKDTSDVRCTNGEPPVFVKPEKVVGVIGASGSSVSIMVANILRLFQIPQISYA
STAPELSDDRRYDFFSRVVPPDSFQAQAMVDIVKALGWNYVSTLASEGSYGEKGVESFTQ
ISKEAGGLCIAQSVRIPQERKDRTIDFDRIIKQLLDTPNSRAVVIFANDEDIKQILAAAK
RADQVGHFLWVGSDSWGSKINPLHQHEDIAEGAITIQPKRATVEGFDAYFTSRTLENNRR
NVWFAEYWEENFNCKLTISGSKKEDTDRKCTGQERIGKDSNYEQEGKVQFVIDAVYAMAH
ALHHMNKDLCADYRGVCPEMEQAGGKKLLKYIRNVNFNGSAGTPVMFNKNGDAPGRYDIF
QYQTTNTSNPGYRLIGQWTDELQLNIEDMQWGKGVREIPASVCTLPCKPGQRKKTQKGTP
CCWTCEPCDGYQYQFDEMTCQHCPYDQRPNENRTGCQDIPIIKLEWHSPWAVIPVFLAML
GIIATIFVMATFIRYNDTPIVRASGRELSYVLLTGIFLCYIITFLMIAKPDVAVCSFRRV
FLGLGMCISYAALLTKTNRIYRIFEQGKKSVTAPRLISPTSQLAITSSLISVQLLGVFIW
FGVDPPNIIIDYDEHKTMNPEQARGVLKCDITDLQIICSLGYSILLMVTCTVYAIKTRGV
PENFNEAKPIGFTMYTTCIVWLAFIPIFFGTAQSAEKLYIQTTTLTISMNLSASVALGML
YMPKVYIIIFHPELNVQKRKRSFKAVVTAATMSSRLSHKPSDRPNGEAKTELCENVDPNS
PAAKKKYVSYNNLVI
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, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. G-protein coupled receptor for glutamate.
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
Glutamatergic synapse (hsa04724 )
Reactome Pathway
Class C/3 (Metabotropic glutamate/pheromone receptors) (R-HSA-420499 )
G alpha (i) signalling events (R-HSA-418594 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
19 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(+)-MCPG DMG5QJB Discovery agent N.A. Investigative [1]
(1S,3R)-ACPD DM5DOAF Discovery agent N.A. Investigative [1]
ADX71743 DM3WAG6 Discovery agent N.A. Investigative [2]
alpha-methylserine-O-phosphate DMCIH1X Discovery agent N.A. Investigative [1]
AMN082 DMXDUCP Discovery agent N.A. Investigative [3]
L-AP4 DMPJFGI Discovery agent N.A. Investigative [1]
L-CCG-I DMPZ8XH Discovery agent N.A. Investigative [1]
L-serine-O-phosphate DMTJ1NH Discovery agent N.A. Investigative [1]
LSP1-2111 DM74J10 Discovery agent N.A. Investigative [4]
LSP4-2022 DMBWHGP Discovery agent N.A. Investigative [5]
MAP4 DMUCE93 Discovery agent N.A. Investigative [1]
MCCG DMKTX1A Discovery agent N.A. Investigative [1]
MMPIP DMWMZL7 Discovery agent N.A. Investigative [6]
MPPG DMJHQ9T Discovery agent N.A. Investigative [1]
MSOPPE DMU67CE Discovery agent N.A. Investigative [1]
PPG DM5IG4F Discovery agent N.A. Investigative [1]
XAP044 DMLTVI6 Discovery agent N.A. Investigative [7]
[3H]LY341495 DMGX0Y8 Discovery agent N.A. Investigative [1]
[3H]quisqualate DMDQBTX Discovery agent N.A. Investigative [8]
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⏷ Show the Full List of 19 Investigative Drug(s)

References

1 Binding of [3H](2S,1'S,2'S)-2-(9-xanthylmethyl)-2-(2'-carboxycyclopropyl) glycine ([3H]LY341495) to cell membranes expressing recombinant human group III metabotropic glutamate receptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2000 Dec;362(6):546-54.
2 ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization. J Pharmacol Exp Ther. 2013 Mar;344(3):624-36.
3 A selective metabotropic glutamate receptor 7 agonist: activation of receptor signaling via an allosteric site modulates stress parameters in vivo. Proc Natl Acad Sci U S A. 2005 Dec 20;102(51):18712-7.
4 Electrophysiological and behavioral evidence that modulation of metabotropic glutamate receptor 4 with a new agonist reverses experimental parkinsonism. FASEB J. 2009 Oct;23(10):3619-28.
5 A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential. FASEB J. 2012 Apr;26(4):1682-93.
6 Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7. Mol Pharmacol. 2010 Mar;77(3):459-68.
7 Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior. J Biol Chem. 2014 Apr 18;289(16):10975-87.
8 Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)... J Med Chem. 1998 Mar 12;41(6):930-9.