Details of the Drug Therapeutic Target (DTT)

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
• 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.
• 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

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]

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.