Details of the Drug Therapeutic Target (DTT)

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

DTT Name N-arachidonyl glycine receptor (GPR18)
Synonyms NAGly receptor; GPCRW; G-protein coupled receptor 18
Gene Name GPR18
DTT Type
Literature-reported target
 [1]
UniProt ID
GPR18_HUMAN
TTD ID
T72267
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MITLNNQDQPVPFNSSHPDEYKIAALVFYSCIFIIGLFVNITALWVFSCTTKKRTTVTIY
MMNVALVDLIFIMTLPFRMFYYAKDEWPFGEYFCQILGALTVFYPSIALWLLAFISADRY
MAIVQPKYAKELKNTCKAVLACVGVWIMTLTTTTPLLLLYKDPDKDSTPATCLKISDIIY
LKAVNVLNLTRLTFFFLIPLFIMIGCYLVIIHNLLHGRTSKLKPKVKEKSIRIIITLLVQ
VLVCFMPFHICFAFLMLGTGENSYNPWGAFTTFLMNLSTCLDVILYYIVSKQFQARVISV
MLYRNYLRSMRRKSFRSGSLRSLSNINSEML
Function
Receptor for endocannabinoid N-arachidonyl glycine (NAGly). However, conflicting results about the role of NAGly as an agonist are reported. Can also be activated by plant-derived and synthetic cannabinoid agonists. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. May contribute to regulation of the immune system. Is required for normal homeostasis of CD8+ subsets of intraepithelial lymphocytes (IELs) (CD8alphaalpha and CD8alphabeta IELs)in small intstine by supporting preferential migration of CD8alphaalpha T-cells to intraepithelial compartment over lamina propria compartment, and by mediating their reconstitution into small intestine after bone marrow transplant (By similarity). Plays a role in hypotensive responses, mediating reduction in intraocular and blood pressure (By similarity). Mediates NAGly-induced process of reorganization of actin filaments and induction of acrosomal exocytosis.
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
Class A/1 (Rhodopsin-like receptors) (R-HSA-373076 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
4 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
abnormal cannabidiol DMV6DAO Discovery agent N.A. Investigative [2]
arachidonylcyclopropylamide DMZM5KE Discovery agent N.A. Investigative [2]
N-arachidonoylglycine DM85RJ1 Discovery agent N.A. Investigative [1]
O-1602 DM9VISB Discovery agent N.A. Investigative [2]
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References

1 Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18. Biochem Biophys Res Commun. 2006 Sep 1;347(3):827-32.
2 Delta(9) -Tetrahydrocannabinol and N-arachidonyl glycine are full agonists at GPR18 receptors and induce migration in human endometrial HEC-1B cells. Br J Pharmacol. 2012 Apr;165(8):2414-24.