Tclin TBXA2R Thromboxane A2 receptor

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / Thromboxane A2 Receptor

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Thromboxane A2 Receptor

Protein Summary

Description

Receptor for thromboxane A2 (TXA2), a potent stimulator of platelet aggregation. The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system. In the kidney, the binding of TXA2 to glomerular TP receptors causes intense vasoconstriction. Activates phospholipase C. Isoform 1 activates adenylyl cyclase. Isoform 2 inhibits adenylyl cyclase. This gene encodes a member of the G protein-coupled receptor family. The protein interacts with thromboxane A2 to induce platelet aggregation and regulate hemostasis. A mutation in this gene results in a bleeding disorder. Multiple transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Oct 2009]

Uniprot Accession IDs

• P21731
• O75228
• Q6DK52
• Q9UCY1
• Q9UCY2
• TXA2-R

Gene Name

• TBXA2R

Ensembl ID

• ENST00000375190
• ENSP00000364336
• ENSG00000006638
• ENST00000411851
• ENSP00000393333

Symbol

• TXA2-R
• BDPLT13

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (chemical)	0.96
histone modification site profile	0.81
kinase	0.72
tissue sample	0.69
biological term	0.67

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 141.04   (req: < 5)

Gene RIFs: 98   (req: <= 3)

Antibodies: 170   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 141.04   (req: >= 5)

Gene RIFs: 98   (req: > 3)

Antibodies: 170   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 16

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 319

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 4

Approved Drugs (4)

Explore Approved Drugs

1 – 4 of 4

dinoprostone

TBXA2RTclin GPCR

: 4.5

dinoprost

TBXA2RTclin GPCR

: 5.1

ramatroban

TBXA2RTclin GPCR

INVERSE AGONIST Ki: 9.24

laropiprant

TBXA2RTclin GPCR

Ki: 8.53

Active Ligands (319)

Explore Active Ligands

1 – 10 of 319

CHEMBL521784

TBXA2RTclin GPCR

Ki: 8.26

iloprost

TBXA2RTclin GPCR

: 5.2

MB-28767

TBXA2RTclin GPCR

: 6.5

carbacyclin

TBXA2RTclin GPCR

: 4.7

CHEMBL1628262

TBXA2RTclin GPCR

: 4.7

CHEMBL65414

TBXA2RTclin GPCR

IC50: 8.22

CHEMBL37853

TBXA2RTclin GPCR

: 5.2

CHEMBL3906016

TBXA2RTclin GPCR

EC50: 7

CHEMBL308351

TBXA2RTclin GPCR

Ki: 7.33

CHEMBL362543

TBXA2RTclin GPCR

Ki: 7

Protein Data Bank (1)

1 – 1 of 1

PDB Structure Id	Ligand	Method	Resolution (Å)	M.W. (kDa)	Pub Year	Title

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (20)

Reactome (13)

KEGG (3)

PathwayCommons (1)

WikiPathways (3)

Class A/1 (Rhodopsin-like receptors) (R-HSA-373076)

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Items per page:

5

1 – 5 of 13

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
Reactome	Eicosanoid ligand-binding receptors	15 targets	R-HSA-391903
Reactome	G alpha (12/13) signalling events	80 targets	R-HSA-416482
Reactome	G alpha (q) signalling events	219 targets	R-HSA-416476
Reactome	GPCR downstream signalling	1152 targets	R-HSA-388396

Name	Explore in Pharos	Explore in Source
Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
Eicosanoid ligand-binding receptors	15 targets	R-HSA-391903
G alpha (12/13) signalling events	80 targets	R-HSA-416482
G alpha (q) signalling events	219 targets	R-HSA-416476
GPCR downstream signalling	1152 targets	R-HSA-388396

Gene Ontology Terms (20)

Functions (2)

Components (4)

Processes (14)

Items per page:

10

1 – 2 of 2

GO Term	Evidence	Assigned by
guanyl-nucleotide exchange factor activity	Traceable Author Statement (TAS)	Reactome
thromboxane A2 receptor activity	Traceable Author Statement (TAS)	ProtInc

Protein-Protein Interactions (221)

Explore Interacting Targets

1 – 10 of 221

• See Interactions on String-DB

TGM2

Tchem

Family: Enzyme

Novelty: 0.00048324

Score: 0.986

Data Source: STRINGDB

GNAQ

Tbio

Novelty: 0.00176666

Score: 0.968

Data Source: Reactome,STRINGDB

LTB4R

Tchem

Family: GPCR

Novelty: 0.00174481

Score: 0.957

Data Source: STRINGDB

GNA13

Tbio

Novelty: 0.05970556

Score: 0.955

Data Source: Reactome,STRINGDB

ADRA1B

Tclin

Family: GPCR

Novelty: 0.00098873

Score: 0.953

Data Source: STRINGDB

ARRB2

Tbio

Novelty: 0.00180049

Score: 0.952

Data Source: STRINGDB

GNAI2

Tbio

Novelty: 0.04542644

Score: 0.952

Data Source: STRINGDB

GNB1

Tbio

Novelty: 0.04716243

Score: 0.95

Data Source: Reactome,STRINGDB

GNG2

Tbio

Novelty: 0.08273543

Score: 0.949

Data Source: Reactome,STRINGDB

GRK5

Tchem

Family: Kinase

Novelty: 0.01219315

Score: 0.948

Data Source: STRINGDB

Publication Statistics

PubMed Score  141.04

PubMed score by year

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PubTator Score  205.93

PubTator score by year

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Patents

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Amino Acid Sequence

Residue Counts

Sequence

MWPNGSSLGPCFRPTNITLEERRLIASPWFAASFCVVGLASNLLALSVLAGARQGGSHTRSSFLTFLCGL

1-70

VLTDFLGLLVTGTIVVSQHAALFEWHAVDPGCRLCRFMGVVMIFFGLSPLLLGAAMASERYLGITRPFSR

70-140

PAVASQRRAWATVGLVWAAALALGLLPLLGVGRYTVQYPGSWCFLTLGAESGDVAFGLLFSMLGGLSVGL

140-210

SFLLNTVSVATLCHVYHGQEAAQQRPRDSEVEMMAQLLGIMVVASVCWLPLLVFIAQTVLRNPPAMSPAG

210-280

QLSRTTEKELLIYLRVATWNQILDPWVYILFRRAVLRRLQPRLSTRPRSLSLQPQLTQRSGLQ

280-343

MWPNGSSLGPCFRPTNITLEERRLIASPWFAASFCVVGLASNLLALSVLAGARQGGSHTRSSFLTFLCGLVLTDFLGLLVTGTIVVSQHAALFEWHAVDPGCRLCRFMGVVMIFFGLSPLLLGAAMASERYLGITRPFSRPAVASQRRAWATVGLVWAAALALGLLPLLGVGRYTVQYPGSWCFLTLGAESGDVAFGLLFSMLGGLSVGLSFLLNTVSVATLCHVYHGQEAAQQRPRDSEVEMMAQLLGIMVVASVCWLPLLVFIAQTVLRNPPAMSPAGQLSRTTEKELLIYLRVATWNQILDPWVYILFRRAVLRRLQPRLSTRPRSLSLQPQLTQRSGLQ

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G-protein coupled receptor
Glycoprotein
Membrane