Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTNET8J)

• DTT Name: G-protein coupled receptor 55 (GPR55)
• Synonyms: LPIR1
• Gene Name: GPR55
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: GPR55_HUMAN
• TTD ID: T87670
• Sequence:
  MSQQNTSGDCLFDGVNELMKTLQFAVHIPTFVLGLLLNLLAIHGFSTFLKNRWPDYAATS
  IYMINLAVFDLLLVLSLPFKMVLSQVQSPFPSLCTLVECLYFVSMYGSVFTICFISMDRF
  LAIRYPLLVSHLRSPRKIFGICCTIWVLVWTGSIPIYSFHGKVEKYMCFHNMSDDTWSAK
  VFFPLEVFGFLLPMGIMGFCCSRSIHILLGRRDHTQDWVQQKACIYSIAASLAVFVVSFL
  PVHLGFFLQFLVRNSFIVECRAKQSISFFLQLSMCFSNVNCCLDVFCYYFVIKEFRMNIR
  AHRPSRVQLVLQDTTISRG
• Function: Receptor for L-alpha-lysophosphatidylinositol (LPI). LPI induces Ca(2+) release from intracellular stores via the heterotrimeric G protein GNA13 and RHOA. Putative cannabinoid receptor. May play a role in bone physiology by regulating osteoclast number and function. May be involved in hyperalgesia associated with inflammatory and neuropathic pain.
• 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

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Guanfacine extended release	DMB1CZ8	Attention deficit hyperactivity disorder	6A05.Z	Approved	[1]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIO-017	DMYHK3Y	Angelman syndrome	LD90.0	Phase 1	[2]

17 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-arachidonoylglycerolphosphoinositol	DMICOL3	Discovery agent	N.A.	Investigative	[3]
2-arachidonyl glyceryl ether	DM2H8TV	Discovery agent	N.A.	Investigative	[1]
abnormal cannabidiol	DMV6DAO	Discovery agent	N.A.	Investigative	[1]
CID1172084	DMK6YOP	Discovery agent	N.A.	Investigative	[4]
CID16020046	DMLWZRT	Discovery agent	N.A.	Investigative	[5]
CID1792197	DMEGZY7	Discovery agent	N.A.	Investigative	[4]
CID2440433	DMA3F7S	Discovery agent	N.A.	Investigative	[4]
CP55,244	DMKWB31	Discovery agent	N.A.	Investigative	[6]
CP55,667	DMNLD6E	Discovery agent	N.A.	Investigative	[6]
GSK494581A	DMMIWHV	Discovery agent	N.A.	Investigative	[6]
GSK575594A	DM1I0AN	Discovery agent	N.A.	Investigative	[6]
lysophosphatidylinositol	DMETM3R	Discovery agent	N.A.	Investigative	[7]
N-oleoylethanolamide	DMJQ4L7	Discovery agent	N.A.	Investigative	[1]
O-1602	DM9VISB	Discovery agent	N.A.	Investigative	[8]
O-arachidonoyl ethanolamine	DML0P72	Discovery agent	N.A.	Investigative	[1]
T1117	DMSA3U4	Discovery agent	N.A.	Investigative	[9]
[3H]CP55940	DMU7FC5	Discovery agent	N.A.	Investigative	[1]

References

• [1] The orphan receptor GPR55 is a novel cannabinoid receptor. Br J Pharmacol. 2007 Dec;152(7):1092-101.
• [2] Clinical pipeline report, company report or official report of Biom Therapeutics
• [3] 2-Arachidonoyl-sn-glycero-3-phosphoinositol: a possible natural ligand for GPR55. J Biochem. 2009 Jan;145(1):13-20.
• [4] Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2011 Jun 28;50(25):5633-47.
• [5] A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther. 2013 Jul;346(1):54-66.
• [6] Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist. J Pharmacol Exp Ther. 2011 Apr;337(1):236-46.
• [7] Screening beta-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors. J Biomol Screen. 2013 Jun;18(5):599-609.
• [8] International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB and CB Pharmacol Rev. 2010 Dec;62(4):588-631.
• [9] Fluorescent ligand binding reveals heterogeneous distribution of adrenoceptors and 'cannabinoid-like' receptors in small arteries. Br J Pharmacol. 2010 Feb;159(4):787-96.