INT91413

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Context Info
Confidence 0.58
First Reported 2000
Last Reported 2010
Negated 0
Speculated 2
Reported most in Abstract
Documents 35
Total Number 50
Disease Relevance 17.94
Pain Relevance 12.03

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

isomerase activity (PTGES) signal transduction (PTGES) cytoplasm (PTGES)
Anatomy Link Frequency
chondrocytes 1
blood 1
plasma 1
monocytes 1
PTGES (Homo sapiens)
Pain Link Frequency Relevance Heat
Inflammation 250 99.92 Very High Very High Very High
cINOD 145 99.92 Very High Very High Very High
COX2 25 99.80 Very High Very High Very High
cOX1 4 99.80 Very High Very High Very High
Pain 64 98.40 Very High Very High Very High
Potency 42 98.20 Very High Very High Very High
IPN 6 98.10 Very High Very High Very High
rheumatoid arthritis 22 97.66 Very High Very High Very High
Osteoarthritis 94 97.36 Very High Very High Very High
Hyperalgesia 33 97.32 Very High Very High Very High
Disease Link Frequency Relevance Heat
INFLAMMATION 336 99.92 Very High Very High Very High
Pain 78 98.40 Very High Very High Very High
Disease 68 98.40 Very High Very High Very High
Atherosclerosis 28 98.40 Very High Very High Very High
Inflammatory Pain 6 98.10 Very High Very High Very High
Rheumatoid Arthritis 22 97.66 Very High Very High Very High
Osteoarthritis 116 97.36 Very High Very High Very High
Hyperalgesia 33 97.32 Very High Very High Very High
Increased Venous Pressure Under Development 2 97.20 Very High Very High Very High
Stroke 16 96.44 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Pharmacological inhibitors of mPGES-1 are proposed as an alternative to nonsteroidal anti-inflammatory drugs.
Negative_regulation (inhibitors) of mPGES-1 associated with inflammation and cinod
1) Confidence 0.58 Published 2010 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 19934399 Disease Relevance 0.10 Pain Relevance 0.10
Taken together, these results indicate that YS121 is a promising inhibitor of mPGES-1 with anti-inflammatory efficiency in human whole blood as well as in vivo.
Negative_regulation (inhibitor) of mPGES-1 in blood associated with inflammation
2) Confidence 0.58 Published 2010 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 19934399 Disease Relevance 0.19 Pain Relevance 0.05
Both active and selective mPGES-1 inhibitors (26 and 44) have a relatively distinct pharmacokinetic profile and are suitable for clinical development.
Negative_regulation (inhibitors) of mPGES-1
3) Confidence 0.58 Published 2009 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 19748780 Disease Relevance 0.10 Pain Relevance 0.19
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
Negative_regulation (inhibitors) of mPGES-1
4) Confidence 0.58 Published 2009 Journal Bioorg. Med. Chem. Lett. Section Title Doc Link 19748780 Disease Relevance 0.09 Pain Relevance 0.17
Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors.
Negative_regulation (inhibitors) of mPGES-1
5) Confidence 0.58 Published 2009 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 19748780 Disease Relevance 0.08 Pain Relevance 0.16
Phenanthrene imidazole 3 (MF63) has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor.
Negative_regulation (inhibitor) of mPGES-1
6) Confidence 0.58 Published 2007 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 18029174 Disease Relevance 0 Pain Relevance 0.15
This profile of mPGES-1 inhibition, distinct from COX-2 inhibition in cells, validates mPGES-1 as an attractive target for therapeutic intervention.
Negative_regulation (inhibition) of mPGES-1
7) Confidence 0.57 Published 2010 Journal Biochem. Pharmacol. Section Abstract Doc Link 20067770 Disease Relevance 0.35 Pain Relevance 0.27
Toward this aim, we identified PF-9184 as a novel mPGES-1 inhibitor.
Negative_regulation (inhibitor) of mPGES-1
8) Confidence 0.57 Published 2010 Journal Biochem. Pharmacol. Section Abstract Doc Link 20067770 Disease Relevance 0.62 Pain Relevance 0.39
The efficacy of nonsteroidal anti-inflammatory drugs and COX-2 inhibitors in the treatment of the signs and symptoms of osteoarthritis, rheumatoid arthritis and inflammatory pain, largely attributed to the inhibition of PGE(2) synthesis, provides a rationale for exploring mPGES-1 inhibition as a potential novel therapy for these diseases.
Negative_regulation (inhibition) of mPGES-1 associated with inflammation, ipn, rheumatoid arthritis, cinod, cox-2 inhibitor, disease and osteoarthritis
9) Confidence 0.57 Published 2010 Journal Biochem. Pharmacol. Section Abstract Doc Link 20067770 Disease Relevance 0.65 Pain Relevance 0.42
Elucidation of the biology of this pathway using diversified approaches is also relevant to understanding the implications of substrate rediversion following inhibition of enzymes downstream of COXs, such as the microsomal PGE synthase (mPGES)-1 and of combining D prostanoid antagonism with niacin to attenuate facial flushing.
Negative_regulation (inhibition) of microsomal PGE synthase associated with increased venous pressure under development
10) Confidence 0.57 Published 2009 Journal J. Thromb. Haemost. Section Abstract Doc Link 19630805 Disease Relevance 0.47 Pain Relevance 0.28
Elucidation of the biology of this pathway using diversified approaches is also relevant to understanding the implications of substrate rediversion following inhibition of enzymes downstream of COXs, such as the microsomal PGE synthase (mPGES)-1 and of combining D prostanoid antagonism with niacin to attenuate facial flushing.
Negative_regulation (inhibition) of mPGES associated with increased venous pressure under development
11) Confidence 0.49 Published 2009 Journal J. Thromb. Haemost. Section Abstract Doc Link 19630805 Disease Relevance 0.47 Pain Relevance 0.28
Our data give evidence for the location of the active site at the interface between subunits in the homotrimeric enzyme and suggest a model of how the natural substrate PGH(2), or competitive inhibitors of MPGES1, enter the active site via the phospholipid bilayer of the membrane.
Negative_regulation (inhibitors) of MPGES1
12) Confidence 0.49 Published 2010 Journal J. Biol. Chem. Section Abstract Doc Link 20605783 Disease Relevance 0.11 Pain Relevance 0.14
A statistically significant inhibition of mPGES-1 activity was detected at 10 and 100microM (38+/-14%, P<0.05, and 69+/-5%, P<0.01, respectively).
Negative_regulation (inhibition) of mPGES-1
13) Confidence 0.43 Published 2010 Journal Biochem. Pharmacol. Section Abstract Doc Link 19925781 Disease Relevance 0.05 Pain Relevance 0
Inhibitors of microsomal prostaglandin (PG) E synthase-1 (mPGES-1) are being developed for the relief of pain.
Negative_regulation (Inhibitors) of mPGES-1 associated with pain
14) Confidence 0.43 Published 2010 Journal Biochem. Pharmacol. Section Abstract Doc Link 19925781 Disease Relevance 0.19 Pain Relevance 0.10
In conclusion, AF3442 is a selective mPGES-1 inhibitor which reduced monocyte PGE(2) generation also in the presence of plasma proteins.
Negative_regulation (inhibitor) of mPGES-1 in plasma
15) Confidence 0.43 Published 2010 Journal Biochem. Pharmacol. Section Abstract Doc Link 19925781 Disease Relevance 0 Pain Relevance 0
Pharmacological inhibition of mPGES-1 did not translate into redirection of PGH(2) metabolism towards other terminal PG synthases in monocytes.
Negative_regulation (inhibition) of mPGES-1 in monocytes
16) Confidence 0.43 Published 2010 Journal Biochem. Pharmacol. Section Abstract Doc Link 19925781 Disease Relevance 0 Pain Relevance 0
We recently presented the design and synthesis of a series of pirinixic acid derivatives that dually inhibit mPGES-1 and 5-lipoxygenase.
Negative_regulation (inhibit) of mPGES-1
17) Confidence 0.43 Published 2010 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 19934399 Disease Relevance 0.10 Pain Relevance 0.10
Here, we investigated the mechanism of mPGES-1 inhibition, the selectivity profile, and the in vivo activity of alpha-(n-hexyl)-substituted pirinixic acid [YS121; 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid)] as a lead compound.
Spec (investigated) Negative_regulation (inhibition) of mPGES-1
18) Confidence 0.43 Published 2010 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 19934399 Disease Relevance 0.09 Pain Relevance 0.09
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Negative_regulation (inhibitors) of mPGES-1
19) Confidence 0.43 Published 2007 Journal Bioorg. Med. Chem. Lett. Section Title Doc Link 18029174 Disease Relevance 0 Pain Relevance 0.16
Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor.
Negative_regulation (inhibition) of mPGES-1 associated with cox2
20) Confidence 0.42 Published 2010 Journal Biochem. Pharmacol. Section Title Doc Link 20067770 Disease Relevance 0.58 Pain Relevance 0.53

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