Target Information
| Target General Information | Top | |||||
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| Target ID |
T87670
(Former ID: TTDNR00683)
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| Target Name |
G-protein coupled receptor 55 (GPR55)
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| Synonyms |
LPIR1
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| Gene Name |
GPR55
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Attention deficit hyperactivity disorder [ICD-11: 6A05] | |||||
| 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.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MSQQNTSGDCLFDGVNELMKTLQFAVHIPTFVLGLLLNLLAIHGFSTFLKNRWPDYAATS
IYMINLAVFDLLLVLSLPFKMVLSQVQSPFPSLCTLVECLYFVSMYGSVFTICFISMDRF LAIRYPLLVSHLRSPRKIFGICCTIWVLVWTGSIPIYSFHGKVEKYMCFHNMSDDTWSAK VFFPLEVFGFLLPMGIMGFCCSRSIHILLGRRDHTQDWVQQKACIYSIAASLAVFVVSFL PVHLGFFLQFLVRNSFIVECRAKQSISFFLQLSMCFSNVNCCLDVFCYYFVIKEFRMNIR AHRPSRVQLVLQDTTISRG Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T58CPZ | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Guanfacine extended release | Drug Info | Approved | Attention deficit hyperactivity disorder | [2] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Agonist | [+] 16 Agonist drugs | + | ||||
| 1 | Guanfacine extended release | Drug Info | [1] | |||
| 2 | 2-arachidonoylglycerolphosphoinositol | Drug Info | [3] | |||
| 3 | 2-arachidonyl glyceryl ether | Drug Info | [1] | |||
| 4 | abnormal cannabidiol | Drug Info | [1] | |||
| 5 | CID1172084 | Drug Info | [4] | |||
| 6 | CID1792197 | Drug Info | [4] | |||
| 7 | CID2440433 | Drug Info | [4] | |||
| 8 | CP55,244 | Drug Info | [6] | |||
| 9 | GSK494581A | Drug Info | [6] | |||
| 10 | GSK575594A | Drug Info | [6] | |||
| 11 | lysophosphatidylinositol | Drug Info | [7] | |||
| 12 | N-oleoylethanolamide | Drug Info | [1] | |||
| 13 | O-1602 | Drug Info | [8] | |||
| 14 | O-arachidonoyl ethanolamine | Drug Info | [1] | |||
| 15 | T1117 | Drug Info | [9] | |||
| 16 | [3H]CP55940 | Drug Info | [1] | |||
| Antagonist | [+] 2 Antagonist drugs | + | ||||
| 1 | CID16020046 | Drug Info | [5] | |||
| 2 | CP55,667 | Drug Info | [6] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Class A/1 (Rhodopsin-like receptors) | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | GPCR ligand binding | |||||
| 2 | GPCR downstream signaling | |||||
| 3 | GPCRs, Other | |||||
| References | Top | |||||
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| REF 1 | The orphan receptor GPR55 is a novel cannabinoid receptor. Br J Pharmacol. 2007 Dec;152(7):1092-101. | |||||
| REF 2 | Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. | |||||
| REF 3 | 2-Arachidonoyl-sn-glycero-3-phosphoinositol: a possible natural ligand for GPR55. J Biochem. 2009 Jan;145(1):13-20. | |||||
| REF 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. | |||||
| REF 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. | |||||
| REF 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. | |||||
| REF 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. | |||||
| REF 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. | |||||
| REF 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. | |||||
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