INT23937

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Context Info
Confidence 0.65
First Reported 1987
Last Reported 2011
Negated 0
Speculated 1
Reported most in Body
Documents 103
Total Number 104
Disease Relevance 55.63
Pain Relevance 24.67

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

cell proliferation (EDNRA) signal transduction (EDNRA) aging (EDNRA)
plasma membrane (EDNRA) signal transducer activity (EDNRA)
Anatomy Link Frequency
plasma 5
melanocytes 4
neurons 4
brain 3
ovary 3
EDNRA (Homo sapiens)
Pain Link Frequency Relevance Heat
antagonist 856 100.00 Very High Very High Very High
methotrexate 225 100.00 Very High Very High Very High
Infliximab 20 100.00 Very High Very High Very High
melanocortin 1 receptor 95 99.92 Very High Very High Very High
dorsal root ganglion 484 99.56 Very High Very High Very High
Sciatic nerve 4 99.56 Very High Very High Very High
Central nervous system 32 99.36 Very High Very High Very High
Kappa opioid receptor 7 98.88 Very High Very High Very High
qutenza 904 98.80 Very High Very High Very High
agonist 306 98.64 Very High Very High Very High
Disease Link Frequency Relevance Heat
Cancer 954 100.00 Very High Very High Very High
Obesity 106 99.96 Very High Very High Very High
Pulmonary Hypertension 1342 99.84 Very High Very High Very High
Breast Cancer 97 99.84 Very High Very High Very High
Reprotox - General 1 214 99.76 Very High Very High Very High
Prostate Cancer 17 99.76 Very High Very High Very High
Death 79 99.72 Very High Very High Very High
Papillomavirus Infection 64 99.68 Very High Very High Very High
Increased Venous Pressure Under Development 273 99.64 Very High Very High Very High
Ganglion Cysts 506 99.56 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
When prescribing any ETRA, it is important to be aware of potential interactions with concomitant medications.
Gene_expression (prescribing) of ETRA
1) Confidence 0.65 Published 2007 Journal Vascular Health and Risk Management Section Body Doc Link PMC1994033 Disease Relevance 0.32 Pain Relevance 0
Sitaxsentan was the first ET-A specific receptor antagonist for the treatment of PAH.
Gene_expression (antagonist) of ET-A associated with pulmonary hypertension and antagonist
2) Confidence 0.65 Published 2010 Journal Vascular Health and Risk Management Section Body Doc Link PMC3004515 Disease Relevance 0.43 Pain Relevance 0.08
ET-A is found primarily on vascular smooth muscle cells and leads to vasoconstriction, proliferation, and fibrosis.
Gene_expression (found) of ET-A in smooth muscle cells associated with fibrosis and increased venous pressure under development
3) Confidence 0.65 Published 2010 Journal Vascular Health and Risk Management Section Body Doc Link PMC3004515 Disease Relevance 0.82 Pain Relevance 0.15
We analyzed the pharmacological properties of 17-cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6b eta-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride (TRK-820) using Chinese hamster ovary (CHO) cells expressing cloned rat mu-, delta- and kappa-opioid receptors and human nociceptin receptor.
Gene_expression (expressing) of eta in CHO associated with orphanin and kappa opioid receptor
4) Confidence 0.65 Published 1999 Journal Eur. J. Pharmacol. Section Abstract Doc Link 10440101 Disease Relevance 0 Pain Relevance 0.35
Whereas ETA receptor expression at both protein and mRNA levels was not affected by IL-1beta treatment, we demonstrated an unexpected predominance of the ETB receptor subtype under this inflammatory condition.
Gene_expression (expression) of ETA associated with inflammation
5) Confidence 0.65 Published 2005 Journal Endocrinology Section Abstract Doc Link 16109787 Disease Relevance 0.19 Pain Relevance 0.18
Alterations in the distribution and number of ETA and ETB receptors in conditions such as PAH suggest that their roles in the disease state may differ from those in normal physiology.
Gene_expression (receptors) of ETA associated with pulmonary hypertension and disease
6) Confidence 0.54 Published 2008 Journal European Heart Journal Section Body Doc Link PMC2515885 Disease Relevance 0.98 Pain Relevance 0.06
Receptor selectivity and endothelin plasma levels
Gene_expression (levels) of endothelin plasma in plasma
7) Confidence 0.54 Published 2008 Journal European Heart Journal Section Body Doc Link PMC2515885 Disease Relevance 0.57 Pain Relevance 0.09
Endothelin-receptor selectivity and its vasoconstriction and vasodilation effects
Gene_expression (selectivity) of Endothelin-receptor associated with increased venous pressure under development
8) Confidence 0.54 Published 2008 Journal European Heart Journal Section Body Doc Link PMC2515885 Disease Relevance 0.87 Pain Relevance 0.12
Endothelin-receptor selectivity and drug efficacy
Gene_expression (selectivity) of Endothelin-receptor
9) Confidence 0.54 Published 2008 Journal European Heart Journal Section Body Doc Link PMC2515885 Disease Relevance 0.76 Pain Relevance 0
Hence, it is not possible to comment on whether ET receptor expression was related to response to treatment.
Spec (whether) Gene_expression (expression) of ET receptor
10) Confidence 0.51 Published 2010 Journal Mol Cancer Section Body Doc Link PMC2856553 Disease Relevance 0.99 Pain Relevance 0
ET-1 and its receptors, ETAR and ETBR, are overexpressed in breast carcinomas.
Gene_expression (overexpressed) of ETAR associated with breast cancer
11) Confidence 0.50 Published 2004 Journal J Transl Med Section Body Doc Link PMC436068 Disease Relevance 1.60 Pain Relevance 0.10
Binding studies show that HPV-infected cells express increased numbers of functional ETAR, and a specific antagonist of ETA inhibits ET-1-induced proliferation.
Gene_expression (express) of ETAR associated with papillomavirus infection and antagonist
12) Confidence 0.50 Published 2004 Journal J Transl Med Section Body Doc Link PMC436068 Disease Relevance 2.18 Pain Relevance 0.14
Increased ETAR expression is also seen with advancing tumor stage and grade in both primary and metastatic prostate cancer.
Gene_expression (expression) of ETAR associated with cancer and reprotox - general 1
13) Confidence 0.50 Published 2004 Journal J Transl Med Section Body Doc Link PMC436068 Disease Relevance 1.24 Pain Relevance 0.04
Transformed melanocytes express both ETAR and ETBR.
Gene_expression (express) of ETAR in melanocytes
14) Confidence 0.50 Published 2004 Journal J Transl Med Section Body Doc Link PMC436068 Disease Relevance 1.64 Pain Relevance 0.13
Human papillomavirus (HPV)-positive human cervical carcinoma cell lines overexpress ET-1 and ETAR mRNA and secrete ET-1 protein compared to HPV-negative cells.
Gene_expression (overexpress) of ETAR mRNA associated with papillomavirus infection and reprotox - general 1
15) Confidence 0.50 Published 2004 Journal J Transl Med Section Body Doc Link PMC436068 Disease Relevance 2.32 Pain Relevance 0.13
Activation of ETA receptors mediates vasoconstriction,4 proliferation,17,18 hypertrophy,5,19 cell migration,20 and fibrosis, whereas activation of endothelial ETB receptors stimulates the release of potent vasodilators (NO and prostacyclin), which exhibit anti-proliferative properties, and prevents apoptosis.21 Importantly, ETB receptors on endothelial cells mediate the clearance of circulating ET-1 in the lungs, kidney, and liver, with up to 50% of mature ET-1 in healthy subjects and 40% in patients with PAH cleared via pulmonary ETB receptors.22 Endothelial cell ETB-receptor activation also inhibits ET converting enzyme-1, the enzyme that is required to produce mature ET-1.23
Gene_expression (produce) of ET in Endothelial cell associated with fibrosis, pulmonary hypertension, hypertrophy, apoptosis and increased venous pressure under development
16) Confidence 0.47 Published 2008 Journal European Heart Journal Section Body Doc Link PMC2515885 Disease Relevance 0.90 Pain Relevance 0.04
For example, the ETRA ambrisentan has been reported to have an ETA:ETB selectivity ranging from 29:1 for ET-1-mediated contraction in the rat aorta32 to 4000:1 in myocardial membranes.33
Gene_expression (selectivity) of ETRA
17) Confidence 0.47 Published 2008 Journal European Heart Journal Section Body Doc Link PMC2515885 Disease Relevance 0.37 Pain Relevance 0.10
For example, the ETRA ambrisentan has been reported to have an ETA:ETB selectivity ranging from 29:1 for ET-1-mediated contraction in the rat aorta32 to 4000:1 in myocardial membranes.33
Gene_expression (selectivity) of ETA
18) Confidence 0.47 Published 2008 Journal European Heart Journal Section Body Doc Link PMC2515885 Disease Relevance 0.36 Pain Relevance 0.10
In contrast, the expression of ETAR in either sciatic nerves or DRG of diabetic rats was not altered.
Gene_expression (expression) of ETAR in DRG associated with diabetes mellitus and sciatic nerve
19) Confidence 0.45 Published 2006 Journal Exp. Neurol. Section Abstract Doc Link 16806184 Disease Relevance 1.66 Pain Relevance 0.94
These findings demonstrating the antitumor, anti-angiogenic, apoptotic activities of ABT-627 in vivo provide a rationale for the clinical evaluation of this molecule, alone and in combination with other therapies, in patients with ovarian tumors and potentially in other epithelial tumors that overexpress functional ETAR.


Gene_expression (overexpress) of ETAR associated with cancer, ovarian cancer and apoptosis
20) Confidence 0.44 Published 2004 Journal J Transl Med Section Body Doc Link PMC436068 Disease Relevance 1.16 Pain Relevance 0

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