Target General Infomation
Target ID
T61243
Former ID
TTDR00821
Target Name
Metabotropic glutamate receptor 7
Gene Name
GRM7
Synonyms
mGluR7; GRM7
Target Type
Research
Function
G-protein coupled receptor for glutamate. 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.
BioChemical Class
GPCR glutamate
Target Validation
T61243
UniProt ID
Sequence
MVQLRKLLRVLTLMKFPCCVLEVLLCALAAAARGQEMYAPHSIRIEGDVTLGGLFPVHAK
GPSGVPCGDIKRENGIHRLEAMLYALDQINSDPNLLPNVTLGARILDTCSRDTYALEQSL
TFVQALIQKDTSDVRCTNGEPPVFVKPEKVVGVIGASGSSVSIMVANILRLFQIPQISYA
STAPELSDDRRYDFFSRVVPPDSFQAQAMVDIVKALGWNYVSTLASEGSYGEKGVESFTQ
ISKEAGGLCIAQSVRIPQERKDRTIDFDRIIKQLLDTPNSRAVVIFANDEDIKQILAAAK
RADQVGHFLWVGSDSWGSKINPLHQHEDIAEGAITIQPKRATVEGFDAYFTSRTLENNRR
NVWFAEYWEENFNCKLTISGSKKEDTDRKCTGQERIGKDSNYEQEGKVQFVIDAVYAMAH
ALHHMNKDLCADYRGVCPEMEQAGGKKLLKYIRNVNFNGSAGTPVMFNKNGDAPGRYDIF
QYQTTNTSNPGYRLIGQWTDELQLNIEDMQWGKGVREIPASVCTLPCKPGQRKKTQKGTP
CCWTCEPCDGYQYQFDEMTCQHCPYDQRPNENRTGCQDIPIIKLEWHSPWAVIPVFLAML
GIIATIFVMATFIRYNDTPIVRASGRELSYVLLTGIFLCYIITFLMIAKPDVAVCSFRRV
FLGLGMCISYAALLTKTNRIYRIFEQGKKSVTAPRLISPTSQLAITSSLISVQLLGVFIW
FGVDPPNIIIDYDEHKTMNPEQARGVLKCDITDLQIICSLGYSILLMVTCTVYAIKTRGV
PENFNEAKPIGFTMYTTCIVWLAFIPIFFGTAQSAEKLYIQTTTLTISMNLSASVALGML
YMPKVYIIIFHPELNVQKRKRSFKAVVTAATMSSRLSHKPSDRPNGEAKTELCENVDPNS
PAAKKKYVSYNNLVI
Structure
3MQ4
Antagonist (+)-MCPG Drug Info [525945]
alpha-methylserine-O-phosphate Drug Info [525945]
MAP4 Drug Info [525945]
MCCG Drug Info [525945]
MPPG Drug Info [525945]
MSOPPE Drug Info [525945]
[3H]LY341495 Drug Info [525945]
Agonist (1S,3R)-ACPD Drug Info [525945]
L-AP4 Drug Info [525945]
L-CCG-I Drug Info [525945]
L-serine-O-phosphate Drug Info [525945]
LSP1-2111 Drug Info [530212]
LSP4-2022 Drug Info [531757]
PPG Drug Info [525945]
Modulator (allosteric modulator) ADX71743 Drug Info [532163]
AMN082 Drug Info [527924]
MMPIP Drug Info [530592]
XAP044 Drug Info [532694]
Inhibitor QUISQUALATE Drug Info [534590]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Glutamatergic synapse
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Metabotropic glutamate receptor group III pathway
Reactome G alpha (i) signalling events
Class C/3 (Metabotropic glutamate/pheromone receptors)
WikiPathways GPCRs, Class C Metabotropic glutamate, pheromone
GPCR ligand binding
GPCR downstream signaling
References
Ref 525945Binding 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.
Ref 527924A 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. Epub 2005 Dec 9.
Ref 530212Electrophysiological 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.
Ref 530592Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7. Mol Pharmacol. 2010 Mar;77(3):459-68.
Ref 531757A 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.
Ref 532163ADX71743, 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.
Ref 532694Blocking 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.
Ref 534590J Med Chem. 1998 Mar 12;41(6):930-9.Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid.

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