INT331336

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Context Info
Confidence 0.03
First Reported 2010
Last Reported 2010
Negated 2
Speculated 0
Reported most in Body
Documents 1
Total Number 10
Disease Relevance 1.71
Pain Relevance 0.43

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

Mir483 (Mus musculus)
Pain Link Frequency Relevance Heat
Potency 50 92.00 High High
Bioavailability 20 84.00 Quite High
Inflammation 20 68.48 Quite High
Glutamate 50 46.48 Quite Low
anesthesia 10 35.24 Quite Low
alcohol 20 5.00 Very Low Very Low Very Low
addiction 10 5.00 Very Low Very Low Very Low
Disease Link Frequency Relevance Heat
Disease 160 98.92 Very High Very High Very High
Infection 180 97.96 Very High Very High Very High
American Trypanosomiasis 50 71.88 Quite High
Parasitic Infection 20 68.88 Quite High
INFLAMMATION 20 68.48 Quite High
Parasitemia 10 64.68 Quite High
Death 10 56.20 Quite High
Body Weight 10 49.20 Quite Low
Heart Disease 10 5.00 Very Low Very Low Very Low
Bites And Stings 10 5.00 Very Low Very Low Very Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Preparation, purification and crystallization of cruzain bound to WRR-483
WRR-483 Binding (bound) of
1) Confidence 0.03 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0.26 Pain Relevance 0
Two unique complexes (A and C) of cruzain covalently bound to the inhibitor WRR-483 comprise the crystallographic unit (Figure 3).
WRR-483 Binding (bound) of
2) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0.11 Pain Relevance 0.10
The WRR-483 inhibitor molecule is covalently bound to the active site cysteine via Michael addition, at a distance of 1.84 Å in complex A and 1.83 in complex C (Figure 3b).
WRR-483 inhibitor molecule Binding (bound) of
3) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0 Pain Relevance 0
Overall, the selectivity profile of WRR-483 was comparable to K11777, but WRR-483 had a lower affinity for all proteases except for cathepsin B.


WRR-483 Neg (except) Binding (affinity) of
4) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0.13 Pain Relevance 0.11
WRR-483 has recently completed pharmacokinetic and toxicology studies (SRI international) and was shown to possess a decent pharmacokinetic profile (Cl?
WRR-483 Binding (completed) of
5) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0.21 Pain Relevance 0.11
Overall, the selectivity profile of WRR-483 was comparable to K11777, but WRR-483 had a lower affinity for all proteases except for cathepsin B.


WRR-483 Neg (except) Binding (affinity) of
6) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0.18 Pain Relevance 0.11
The most interesting of interactions, because they are located within the bottom of the S2 pocket, the site known to impact substrate preference profiles for papain-family cysteine proteases, are with the Arg moiety of WRR-483.
WRR-483 Binding (interactions) of
7) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0 Pain Relevance 0
Crystallographic evidence indicates that WRR-483 indeed binds to cruzain in a similar fashion compared to other vinyl sulfone analogs, with the addition of hydrogen bonding interactions between Glu208 in the S2 pocket and the arginine side chain of the inhibitor.
WRR-483 Binding (binds) of
8) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0.10 Pain Relevance 0
Herein, we report the synthesis of WRR-483 (2), the arginine variant of K11777, its remarkable biological properties, and a crystal structure of WRR-483 bound to cruzain.


WRR-483 Binding (bound) of
9) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Body Doc Link PMC2939063 Disease Relevance 0.09 Pain Relevance 0
The crystal structure of WRR-483 bound to cruzain elucidates the details of inhibitor binding to the enzyme.
WRR-483 Binding (bound) of
10) Confidence 0.02 Published 2010 Journal PLoS Neglected Tropical Diseases Section Abstract Doc Link PMC2939063 Disease Relevance 0.64 Pain Relevance 0

General Comments

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