Details of the Target

General Information of Target

Target ID LDTP06218
Target Name Metabotropic glutamate receptor 4 (GRM4)
Gene Name GRM4
Gene ID 2914
Synonyms
GPRC1D; MGLUR4; Metabotropic glutamate receptor 4; mGluR4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPGKRGLGWWWARLPLCLLLSLYGPWMPSSLGKPKGHPHMNSIRIDGDITLGGLFPVHGR
GSEGKPCGELKKEKGIHRLEAMLFALDRINNDPDLLPNITLGARILDTCSRDTHALEQSL
TFVQALIEKDGTEVRCGSGGPPIITKPERVVGVIGASGSSVSIMVANILRLFKIPQISYA
STAPDLSDNSRYDFFSRVVPSDTYQAQAMVDIVRALKWNYVSTVASEGSYGESGVEAFIQ
KSREDGGVCIAQSVKIPREPKAGEFDKIIRRLLETSNARAVIIFANEDDIRRVLEAARRA
NQTGHFFWMGSDSWGSKIAPVLHLEEVAEGAVTILPKRMSVRGFDRYFSSRTLDNNRRNI
WFAEFWEDNFHCKLSRHALKKGSHVKKCTNRERIGQDSAYEQEGKVQFVIDAVYAMGHAL
HAMHRDLCPGRVGLCPRMDPVDGTQLLKYIRNVNFSGIAGNPVTFNENGDAPGRYDIYQY
QLRNDSAEYKVIGSWTDHLHLRIERMHWPGSGQQLPRSICSLPCQPGERKKTVKGMPCCW
HCEPCTGYQYQVDRYTCKTCPYDMRPTENRTGCRPIPIIKLEWGSPWAVLPLFLAVVGIA
ATLFVVITFVRYNDTPIVKASGRELSYVLLAGIFLCYATTFLMIAEPDLGTCSLRRIFLG
LGMSISYAALLTKTNRIYRIFEQGKRSVSAPRFISPASQLAITFSLISLQLLGICVWFVV
DPSHSVVDFQDQRTLDPRFARGVLKCDISDLSLICLLGYSMLLMVTCTVYAIKTRGVPET
FNEAKPIGFTMYTTCIVWLAFIPIFFGTSQSADKLYIQTTTLTVSVSLSASVSLGMLYMP
KVYIILFHPEQNVPKRKRSLKAVVTAATMSNKFTQKGNFRPNGEAKSELCENLEAPALAT
KQTYVTYTNHAI
Target Type
Literature-reported
Target Bioclass
GPCR
Family
G-protein coupled receptor 3 family
Subcellular location
Cell membrane
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. Signaling inhibits adenylate cyclase activity.
TTD ID
T99402
Uniprot ID
Q14833
DrugMap ID
TTICZ1O
Ensemble ID
ENST00000374177.7
HGNC ID
HGNC:4596
ChEMBL ID
CHEMBL2736

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.I503L; p.P544H; p.P854S .
HEC1 SNV: p.I677T; p.L846P .
HT SNV: p.S311A .
HT115 SNV: p.R393Ter .
MCC13 SNV: p.P429L .
MCC26 SNV: p.G36S .
MELJUSO SNV: p.R170C .
MEWO SNV: p.E783V .
NCIH1793 SNV: p.G510A .
NCIH1993 SNV: p.L7F .
NCIH2286 SNV: p.V589L .
NCIH358 SNV: p.S349P .
P31FUJ SNV: p.R554H .
PF382 SNV: p.I802T .
SKMEL24 SNV: p.P577L .
SW403 SNV: p.W314L .
TOV21G SNV: p.R505L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		C435(1.18)  LDD1701  [1]
CY4
 Probe Info  		M869(0.00); S870(0.00); T868(0.00)  LDD0247  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C435(0.93)  LDD1702  [1]
 LDCM0023  KB03 MDA-MB-231 C435(1.18)  LDD1701  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Glutamic Acid Small molecular drug DB00142
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dt-1687 . D0L2YR
Investigative
Click To Hide/Show 27 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(2s,1'r,2's)-2-(2'-phosphonocyclopropyl)Glycine Small molecular drug D0P2VP
(S)-3,4-dcpg Small molecular drug D0LC5O
2-methyl-6-(Phenylethynyl)Pyridine Small molecular drug D0IO8J
Acpt-i Small molecular drug D0W3PY
Adx-88178 Small molecular drug D05GQH
Cppg Small molecular drug D06PHE
Fp0429 Small molecular drug D06DRY
L-ap4 Small molecular drug D0PN6Z
L-ccg-i Small molecular drug D0Z7CZ
L-serine-o-phosphate Small molecular drug D07PZQ
Lsp1-2111 Small molecular drug D0XG6U
Lsp4-2022 Small molecular drug D0KL4K
Lu Af21934 Small molecular drug D0GI1D
Map4 Small molecular drug D09SXN
Mppg Small molecular drug D0D2GL
Phccc Small molecular drug D0H6BG
Pmid20638279c11 Small molecular drug D03PGL
Pmid20638279c7 Small molecular drug D0V8KA
Pmid21688779c22a Small molecular drug D00NCL
Pmid22465637c1 Small molecular drug D0T1SP
Vu0001171 Small molecular drug D0Z5JT
Vu0092145 Small molecular drug D07IOB
Vu0155041 Small molecular drug D0X3VM
Vu0359516 Small molecular drug D09ONV
Vu0361737 Small molecular drug D01JFF
Vu0364770 Small molecular drug D0W9VN
Vu0400195 Small molecular drug D0AY5T

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
2 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.