Target Information

Target General Information

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Target ID

T87670 (Former ID: TTDNR00683)

Target Name

G-protein coupled receptor 55 (GPR55)

Synonyms

LPIR1

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Gene Name

GPR55

Target Type

Successful target

[1]

Disease

[+] 1 Target-related Diseases

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.

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BioChemical Class

GPCR rhodopsin

UniProt ID

GPR55_HUMAN

Sequence

MSQQNTSGDCLFDGVNELMKTLQFAVHIPTFVLGLLLNLLAIHGFSTFLKNRWPDYAATS
IYMINLAVFDLLLVLSLPFKMVLSQVQSPFPSLCTLVECLYFVSMYGSVFTICFISMDRF
LAIRYPLLVSHLRSPRKIFGICCTIWVLVWTGSIPIYSFHGKVEKYMCFHNMSDDTWSAK
VFFPLEVFGFLLPMGIMGFCCSRSIHILLGRRDHTQDWVQQKACIYSIAASLAVFVVSFL
PVHLGFFLQFLVRNSFIVECRAKQSISFFLQLSMCFSNVNCCLDVFCYYFVIKEFRMNIR
AHRPSRVQLVLQDTTISRG

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3D Structure

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AlphaFold

HIT2.0 ID

T58CPZ

Drugs and Modes of Action

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Approved Drug(s)

[+] 1 Approved Drugs

Guanfacine extended release

Drug Info

Approved

Attention deficit hyperactivity disorder

[2]

Clinical Trial Drug(s)

[+] 1 Clinical Trial Drugs

BIO-017

Drug Info

Phase 1

Angelman syndrome

[3]

Mode of Action

[+] 3 Modes of Action

Agonist

[+] 16 Agonist drugs

Guanfacine extended release

Drug Info

[1]

2-arachidonoylglycerolphosphoinositol

Drug Info

[4]

2-arachidonyl glyceryl ether

Drug Info

[1]

abnormal cannabidiol

Drug Info

[1]

CID1172084

Drug Info

[5]

CID1792197

Drug Info

[5]

CID2440433

Drug Info

[5]

CP55,244

Drug Info

[7]

GSK494581A

Drug Info

[7]

GSK575594A

Drug Info

[7]

lysophosphatidylinositol

Drug Info

[8]

N-oleoylethanolamide

Drug Info

[1]

O-1602

Drug Info

[9]

O-arachidonoyl ethanolamine

Drug Info

[1]

T1117

Drug Info

[10]

[3H]CP55940

Drug Info

[1]

Modulator

[+] 1 Modulator drugs

BIO-017

Drug Info

[3]

Antagonist

[+] 2 Antagonist drugs

CID16020046

Drug Info

[6]

CP55,667

Drug Info

[7]

Cell-based Target Expression Variations

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Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database. The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017). Human Similarity Proteins Biological Network Descriptors

Different Human System Profiles of Target

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Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.

The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017).

Human Similarity Proteins

Biological Network Descriptors

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 11A1 (OR11A1)	PF13853	27.132 (35/129)	2.00E-03

Degree	1	Degree centrality	1.07E-04	Betweenness centrality	0.00E+00
Closeness centrality	1.68E-01	Radiality	1.26E+01	Clustering coefficient	0.00E+00
Neighborhood connectivity	7.00E+00	Topological coefficient	1.00E+00	Eccentricity	13
Download	Click to Download the Full PPI Network of This Target

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"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

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Target-regulating microRNAs

Target-regulating microRNAs Info

Target Affiliated Biological Pathways

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Reactome

[+] 2 Reactome Pathways

Class A/1 (Rhodopsin-like receptors)

G alpha (i) signalling events

WikiPathways

[+] 3 WikiPathways

GPCR ligand binding

GPCR downstream signaling

GPCRs, Other

References

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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

Clinical pipeline report, company report or official report of Biom Therapeutics

REF 4

2-Arachidonoyl-sn-glycero-3-phosphoinositol: a possible natural ligand for GPR55. J Biochem. 2009 Jan;145(1):13-20.

REF 5

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 6

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 7

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 8

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 9

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 10

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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