INT122171

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Context Info
Confidence 0.59
First Reported 2005
Last Reported 2010
Negated 0
Speculated 1
Reported most in Abstract
Documents 5
Total Number 6
Disease Relevance 1.92
Pain Relevance 1.22

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

cytosol (AKR1C1) oxidoreductase activity (AKR1C1) cytoplasm (AKR1C1)
AKR1C1 (Homo sapiens)
Pain Link Frequency Relevance Heat
endometriosis 3 97.32 Very High Very High Very High
Dismenorea 3 95.48 Very High Very High Very High
cINOD 10 91.36 High High
alcohol 1 83.52 Quite High
palliative 1 51.68 Quite High
Opioid 1 48.12 Quite Low
antagonist 1 45.92 Quite Low
opioid receptor 1 45.48 Quite Low
Disease Link Frequency Relevance Heat
Endometriosis (extended) 6 98.24 Very High Very High Very High
Disease 5 96.04 Very High Very High Very High
Reprotox - General 1 3 95.48 Very High Very High Very High
Epilepsy 3 94.12 High High
Depressive Disorder 3 93.60 High High
INFLAMMATION 4 85.68 High High
Leukemia 2 76.72 Quite High
Constipation 2 52.76 Quite High
Cancer 2 5.00 Very Low Very Low Very Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Inhibitors of AKR1C1 are thus potential agents for treatment of endometrial cancer and endometriosis, as well as other diseases like premenstrual syndrome, catamenial epilepsy and depressive disorders.We have synthesized a series of pyrimidine, phthalimido and athranilic acid derivatives, and have here examined their inhibitory properties towards AKR1C1.
Spec (examined) Negative_regulation (Inhibitors) of AKR1C1 associated with epilepsy, endometriosis, endometriosis (extended), dismenorea, disease and depressive disorder
1) Confidence 0.59 Published 2009 Journal Chem. Biol. Interact. Section Abstract Doc Link 19007763 Disease Relevance 0.57 Pain Relevance 0.14
Derivatives of pyrimidine, phthalimide and anthranilic acid as inhibitors of human hydroxysteroid dehydrogenase AKR1C1.
Negative_regulation (inhibitors) of AKR1C1
2) Confidence 0.59 Published 2009 Journal Chem. Biol. Interact. Section Title Doc Link 19007763 Disease Relevance 0.41 Pain Relevance 0.10
The AKR1C inhibitor phenolphthalein inhibited MNTX and naltrexone reduction up to 98%. 5beta-Cholanic acid 3alpha,7alpha-diol, the AKR1C2 inhibitor, and medroxyprogesterone acetate, an inhibitor of AKR1C1, AKR1C2, and AKR1C4, inhibited MNTX reduction up to 67%.
Negative_regulation (inhibitor) of AKR1C1
3) Confidence 0.55 Published 2010 Journal Drug Metab. Dispos. Section Abstract Doc Link 20173089 Disease Relevance 0.05 Pain Relevance 0.09
The most potent inhibitors of AKR1C1 were the pyrimidine derivative N-benzyl-2-(2-(4-methoxybenzyl)-6-oxo-1,6-dihydropyrimidin-4-yl)acetamide (K(i)=17 microM) and the anthranilic acid derivative 2-(((2',3-dichlorobiphenyl-4-yl)carbonyl)(methyl)amino)benzoic acid (K(i)=33 microM), both of which are non-competitive inhibitors.
Negative_regulation (inhibitors) of AKR1C1
4) Confidence 0.43 Published 2009 Journal Chem. Biol. Interact. Section Abstract Doc Link 19007763 Disease Relevance 0.51 Pain Relevance 0.13
We report a structural series of N-phenylanthranilic acid derivatives and steroid carboxylates that selectively inhibit recombinant AKR1C isoforms but do not inhibit recombinant COX-1 or COX-2.
Negative_regulation (inhibit) of AKR1C
5) Confidence 0.14 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 15475569 Disease Relevance 0.24 Pain Relevance 0.43
Crystallographic and molecular modeling studies showed that the carboxylic acid of the inhibitor ligand was tethered by the catalytic Tyr55-OH(2)(+) and explained why A-ring substituted N-phenylanthranilates inhibited only AKR1C enzymes.
Negative_regulation (inhibited) of AKR1C
6) Confidence 0.12 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 15475569 Disease Relevance 0.13 Pain Relevance 0.33

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