INT278827

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Context Info
Confidence 0.17
First Reported 2008
Last Reported 2009
Negated 0
Speculated 0
Reported most in Body
Documents 3
Total Number 7
Disease Relevance 2.70
Pain Relevance 0.67

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

extracellular space (EDN1) extracellular region (EDN1) plasma membrane (EDNRB)
signal transducer activity (EDNRB) cell-cell signaling (EDN1) cytoplasm (EDN1)
Anatomy Link Frequency
superior 2
lungs 1
kidney 1
EDN1 (Homo sapiens)
EDNRB (Homo sapiens)
Pain Link Frequency Relevance Heat
antagonist 235 97.48 Very High Very High Very High
cytokine 10 83.28 Quite High
Kinase C 10 78.48 Quite High
Inflammation 12 74.16 Quite High
fibrosis 4 73.48 Quite High
Bioavailability 7 60.32 Quite High
Catecholamine 5 52.24 Quite High
Calcium channel 6 50.28 Quite High
headache 11 5.00 Very Low Very Low Very Low
tolerance 9 5.00 Very Low Very Low Very Low
Disease Link Frequency Relevance Heat
Pulmonary Hypertension 521 98.52 Very High Very High Very High
Increased Venous Pressure Under Development 62 93.80 High High
Apoptosis 10 92.72 High High
Disease 90 74.56 Quite High
INFLAMMATION 12 74.16 Quite High
Fibrosis 2 73.48 Quite High
Natriuresis 10 64.16 Quite High
Stress 15 63.08 Quite High
Hypoxia 5 55.72 Quite High
Hyperplasia 5 55.60 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
ET-1 binds to 2 heptahelical G-protein-coupled receptors, named endothelin receptor-A (ETA) and endothelin receptor-B (ETB).
ET-1 Binding (binds) of ETB
1) Confidence 0.17 Published 2008 Journal Drug design, development and therapy Section Body Doc Link PMC2761178 Disease Relevance 0.66 Pain Relevance 0.05
ET-1 binds to 2 heptahelical G-protein-coupled receptors, named endothelin receptor-A (ETA) and endothelin receptor-B (ETB).
ET-1 Binding (binds) of endothelin receptor-B
2) Confidence 0.17 Published 2008 Journal Drug design, development and therapy Section Body Doc Link PMC2761178 Disease Relevance 0.66 Pain Relevance 0.05
Clearance of ET-1 occurs primarily via binding to ETB, particularly in the vascular beds of the lungs and kidney.
ET-1 Binding (binding) of ETB in kidney
3) Confidence 0.12 Published 2008 Journal Drug design, development and therapy Section Body Doc Link PMC2761178 Disease Relevance 0.09 Pain Relevance 0.08
ET-1 forms an insoluble bond with the ETB that is internalized and degraded (DÂ’Orleans-Juste et al 2002).
ET-1 Binding (bond) of ETB
4) Confidence 0.10 Published 2008 Journal Drug design, development and therapy Section Body Doc Link PMC2761178 Disease Relevance 0.14 Pain Relevance 0.08
Selective agents with relative ETA:ETB affinity of greater than 100:1 have been developed, eg, sitaxentan, relative affinity 6500:1, which have also been shown to reduce endothelin-1 levels.19 Bosentan exhibits a relative ETA:ETB affinity of 20:1 by in vitro assays and is therefore classed as a dual ERA.20 Although ETA selectivity is attractive, these selective agents have not been shown to be superior to bosentan in clinical trials.
endothelin-1 Binding (affinity) of ETB in superior associated with antagonist
5) Confidence 0.06 Published 2009 Journal Vascular Health and Risk Management Section Body Doc Link PMC2725793 Disease Relevance 0.55 Pain Relevance 0.17
Selective agents with relative ETA:ETB affinity of greater than 100:1 have been developed, eg, sitaxentan, relative affinity 6500:1, which have also been shown to reduce endothelin-1 levels.19 Bosentan exhibits a relative ETA:ETB affinity of 20:1 by in vitro assays and is therefore classed as a dual ERA.20 Although ETA selectivity is attractive, these selective agents have not been shown to be superior to bosentan in clinical trials.
endothelin-1 Binding (affinity) of ETB in superior associated with antagonist
6) Confidence 0.06 Published 2009 Journal Vascular Health and Risk Management Section Body Doc Link PMC2725793 Disease Relevance 0.51 Pain Relevance 0.15
Clearance of ET-1 occurs primarily via binding to ETB, particularly in the vascular beds of the lungs and kidney.
ET-1 Binding (binding) of ETB in lungs
7) Confidence 0.04 Published 2008 Journal Drug design, development and therapy Section Body Doc Link PMC2761178 Disease Relevance 0.09 Pain Relevance 0.08

General Comments

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