Property Summary

NCBI Gene PubMed Count 180
Grant Count 95
R01 Count 55
Funding $14,980,988.67
PubMed Score 617.30
PubTator Score 1930.88

Knowledge Summary

Patent (39,709)

TINX Plot

  Disease Relevance (53)

Disease Z-score Confidence
Hypertension 287 5.118 2.6
Systemic scleroderma 66 4.255 2.1
Mandibulofacial dysostosis with alopecia 3 4.184 2.1
Heart disease 279 3.614 1.8
Cancer 2,346 3.408 1.7
Kidney disease 396 3.337 1.7
Portal hypertension 21 3.29 1.6
Scarlet fever 9 3.061 1.5
tuberculosis 1,557 3.001 1.5
Breast cancer 3,094
Congenital Heart Defects 37
Craniofacial Abnormalities 147
Dental caries 67 2.0
Diabetes Mellitus, Non-Insulin-Dependent 157
Diaphragmatic Hernia 40
Endometriosis 535
Erectile dysfunction 10
Hypertensive disease 193
Intracranial aneurysm 20 2.0
Migraine Disorders 26
Nasopharyngeal Neoplasms 8
Pick disease 1,893
Pulmonary hypertension 52
Sleep Apnea, Obstructive 1
Systemic sclerosis 2
X-linked cerebral adrenoleukodystrophy 115
astrocytic glioma 2,241
atypical teratoid / rhabdoid tumor 4,369
autosomal dominant Emery-Dreifuss muscul... 499 
colon cancer 1,475
cystic fibrosis 1,665
gastric carcinoma 832
glioblastoma 5,572
interstitial cystitis 2,299
intraductal papillary-mucinous adenoma (... 2,956 
intraductal papillary-mucinous carcinoma... 2,988 
invasive ductal carcinoma 2,950
lung adenocarcinoma 2,713
lung cancer 4,466
malignant mesothelioma 3,162
medulloblastoma, large-cell 6,234
non-small cell lung cancer 2,798
oligodendroglioma 2,849
osteosarcoma 7,933
ovarian cancer 8,484
pancreatic cancer 2,300
pediatric high grade glioma 2,712
pilocytic astrocytoma 3,086
posterior fossa group A ependymoma 1,511
primary pancreatic ductal adenocarcinoma 1,271
psoriasis 6,685
pulmonary arterial hypertension 36
ulcerative colitis 2,087

Expression

Synonym

Accession P25101 B2R723 B4E2V6 B7Z9G6 D3DP03 E7ER36 O43441 Q16432 Q16433 Q8TBH2
Symbols ETA
ET-A
ETAR
ETRA
MFDA
ETA-R
hET-AR

Gene

PANTHER Protein Class (2)

  TechDev Info (1)

MLP Assay (15)

AID Type Active / Inconclusive / Inactive Description
1788 other 0 / 0 / 0 Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity
1921 other 2 / 0 / 0 Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity
624355 other 0 / 0 / 0 Late stage results from the probe development efforts to identify dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and nuclear factor NF-kappa-B (NF-kB): Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
624406 other 0 / 0 / 0 Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
652083 other 0 / 0 / 0 Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assay
686924 other 0 / 0 / 1 ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound)
686925 other 0 / 0 / 1 ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound)
686926 other 0 / 0 / 1 ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound)
686927 other 0 / 0 / 1 ML353 Eurofin Panel Assay for mGlu5 SAM Inhibitor (Probe Compound)
743249 screening 1 / 0 / 0 Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM)
More...

Gene RIF (159)

PMID Text
26675258 High ETAR expression is associated with ovarian carcinoma.
26357964 Data show that macitentan interferes with the profibrotic action of transforming growth factor-beta (TGF-beta), blocking the endothelin receptor type A (ET-1 receptor) portion of the ET-1/TGF-beta receptor complex.
26176954 Ednra, encoding Endothelin receptor A (ETA)-the target of Endothelin 1 (ET-1)-was significantly increased in Systemic Capillary Leak Syndrome blood-outgrowth endothelial cells compared to healthy controls.
25946671 Endothelin receptor A was detected in all patients with squamous cell carcinoma and psoriasis, with a higher frequency and grade of expression than controls and basal cell carcinoma.
25801761 Plasma proET-1 levels increase in CKD and may be useful biomarkers of renal injury. Increases in response to endothelin A antagonism may reflect EDN1 upregulation, which may partly explain fluid retention with these agents.
25772936 Mutations in the endothelin receptor type A cause mandibulofacial dysostosis with alopecia.
25424718 Genebased analyses revealed associations of the EDNRA gene with longitudinal Blood Pressure phenotypes, associations with essential hypertension, Blood Pressure salt sensitivity, preeclampsia, or preclinical stages of atherosclerosis.
25381251 Data show that upon endothelin-1 (ET-1) stimulation, ET type A receptor (ETAR) is recycled back to plasma membrane, whereas ET type B receptor (ETAR) is targeted to lysosome for degradation.
25377471 our findings reveal the existence of a novel mechanism by which ETAR/beta-arr1 signaling is integrated with the Wnt/beta-catenin pathway to sustain chemoresistance in epithelial ovarian cancer, and they offer a solid rationale for clinical evaluation
25225183 significant single nucleotide polymorphism associations with birth weight near coding regions for two genes involved in oxygen sensing and vascular control, PRKAA1 and EDNRA, respectively, were identified.
More...

AA Sequence

METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCP      1 - 70
QQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFK     71 - 140
LLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLVTAIEIVSIW    141 - 210
ILSFILAIPEAIGFVMVPFEYRGEQHKTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTC    211 - 280
EMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLM    281 - 350
DYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRS    351 - 420
SHKDSMN                                                                   421 - 427
//

Text Mined References (183)

PMID Year Title
26675258 2016 miR-30a inhibits endothelin A receptor and chemoresistance in ovarian carcinoma.
26357964 2015 Macitentan inhibits the transforming growth factor-? profibrotic action, blocking the signaling mediated by the ETR/T?RI complex in systemic sclerosis dermal fibroblasts.
26176954 2015 Endothelial Expression of Endothelin Receptor A in the Systemic Capillary Leak Syndrome.
25946671 2015 Immunohistochemical assessment of endothelin-1 axis in psoriasis, basal cell carcinoma and squamous cell carcinoma.
25801761 2015 Plasma pro-endothelin-1 peptide concentrations rise in chronic kidney disease and following selective endothelin A receptor antagonism.
25772936 2015 Mutations in the endothelin receptor type A cause mandibulofacial dysostosis with alopecia.
25424718 2015 Associations of Endothelial System Genes With Blood Pressure Changes and Hypertension Incidence: The GenSalt Study.
25381251 2014 Agonist-promoted ubiquitination differentially regulates receptor trafficking of endothelin type A and type B receptors.
25377471 2014 Endothelin A receptor/?-arrestin signaling to the Wnt pathway renders ovarian cancer cells resistant to chemotherapy.
25225183 2014 Maternal PRKAA1 and EDNRA genotypes are associated with birth weight, and PRKAA1 with uterine artery diameter and metabolic homeostasis at high altitude.
More...