INT91758

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Context Info
Confidence 0.45
First Reported 2000
Last Reported 2010
Negated 1
Speculated 0
Reported most in Body
Documents 28
Total Number 33
Disease Relevance 20.16
Pain Relevance 7.07

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

endosome (CCR5) plasma membrane (CCR5) cell-cell signaling (CCR5)
cytoplasm (CCR5) signal transducer activity (CCR5)
Anatomy Link Frequency
monocytes 2
memory T cells 2
macrophage 1
lymphocytes 1
T lymphocyte 1
CCR5 (Homo sapiens)
Pain Link Frequency Relevance Heat
antagonist 528 100.00 Very High Very High Very High
chemokine 365 100.00 Very High Very High Very High
cytokine 43 100.00 Very High Very High Very High
opioid receptor 4 99.80 Very High Very High Very High
rheumatoid arthritis 68 99.76 Very High Very High Very High
Inflammation 96 99.20 Very High Very High Very High
addiction 55 98.18 Very High Very High Very High
Morphine 3 98.08 Very High Very High Very High
Chronic pancreatitis 6 94.76 High High
Arthritis 50 92.68 High High
Disease Link Frequency Relevance Heat
Acquired Immune Deficiency Syndrome Or Hiv Infection 2059 100.00 Very High Very High Very High
Disease Progression 50 99.92 Very High Very High Very High
Rheumatoid Arthritis 68 99.76 Very High Very High Very High
INFLAMMATION 99 99.20 Very High Very High Very High
Sprains And Strains 187 99.08 Very High Very High Very High
Infection 553 98.60 Very High Very High Very High
Polymyalgia Rheumatica 228 98.32 Very High Very High Very High
Pancreatitis 22 94.76 High High
Hypersensitivity 31 94.28 High High
Death 17 93.32 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
After interaction with the CC chemokine receptor 5 (CCR5), it activates memory T cells and monocytes, which are the predominant cells in the synovial tissue of patients with PMR [16].
CCR5 Binding (interaction) of in memory T cells associated with chemokine and polymyalgia rheumatica
1) Confidence 0.45 Published 2001 Journal Arthritis Res Section Body Doc Link PMC128892 Disease Relevance 0.96 Pain Relevance 0.16
These results suggest that oligomerization of chemokine receptor CCR5 and opioid receptors on the cell membrane of human or monkey lymphocytes may modulate receptor functions.
chemokine receptor CCR5 Binding (oligomerization) of in lymphocytes associated with chemokine and opioid receptor
2) Confidence 0.42 Published 2002 Journal Exp. Cell Res. Section Abstract Doc Link 12413885 Disease Relevance 0.05 Pain Relevance 0.53
However, two other studies have not confirmed the association of CCR5 with RA [21,22].
CCR5 Neg (not) Binding (association) of associated with rheumatoid arthritis
3) Confidence 0.39 Published 2001 Journal Arthritis Res Section Body Doc Link PMC128892 Disease Relevance 1.24 Pain Relevance 0.33
After interaction with the CC chemokine receptor 5 (CCR5), it activates memory T cells and monocytes, which are the predominant cells in the synovial tissue of patients with PMR [16].
chemokine receptor 5 Binding (interaction) of in memory T cells associated with chemokine and polymyalgia rheumatica
4) Confidence 0.39 Published 2001 Journal Arthritis Res Section Body Doc Link PMC128892 Disease Relevance 0.96 Pain Relevance 0.16
 ; chemokine ligands, CCL4 and CCL7; chemokine receptors, CCR3 and CCR5; and transforming growth factor-beta 2 (TGF-?
CCR5 Binding (receptors) of associated with chemokine
5) Confidence 0.36 Published 2008 Journal Molecular Vision Section Body Doc Link PMC2562425 Disease Relevance 0.07 Pain Relevance 0.10
As is exemplified by CCR5 and its ligands, the host defense mechanism is both complex and redundant.
CCR5 Binding (exemplified) of
6) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.21 Pain Relevance 0.39
These include agents to block CD4 binding by viral gp120, inhibit CCR5 or CXCR4 co-receptor binding by gp120, as well as inhibit gp41 mediated fusion of the viral and cellular lipid bilayers as the Food and Drug Administration (FDA)-approved agent enfuvirtide does (Guo et al 2003; Jacobson et al 2004; Oldfield et al 2005; Kadow et al 2006; Moyle et al 2007).
CCR5 Binding (co-receptor binding) of
7) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.71 Pain Relevance 0.04
As previously discussed, targeting CCR5 leaves a patient without the role of the CCR5 receptor in innate immunity.
CCR5 Binding (targeting) of
8) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.32 Pain Relevance 0.27
As is exemplified by CCR5 and its ligands, the host defense mechanism is both complex and redundant.
CCR5 Binding (ligands) of
9) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.20 Pain Relevance 0.45
Native ligands for CCR5 include chemokines MIP-1?
CCR5 Binding (ligands) of associated with chemokine
10) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.25 Pain Relevance 0.41
The small-molecule antagonists to be discussed bind in a hydrophobic pocket of CCR5 formed by transmembrane helices, and act through allosteric effects.
CCR5 Binding (bind) of associated with antagonist
11) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.39 Pain Relevance 0.20
The ligands for CCR5 and CXCR4 are chemokines, which are small molecules in the cytokine family that promote chemotaxis and cellular activation; on binding to their receptor on the target cell, an intracellular signaling cascade is initiated via a G-protein release from the intracellular domain of the receptor (Oppermann 2004).
CCR5 Binding (binding) of associated with chemokine and cytokine
12) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.26 Pain Relevance 0.35
Those workers found that the allele and genotype frequencies of CCR5?
CCR5 Binding (found) of
13) Confidence 0.35 Published 2001 Journal Arthritis Res Section Body Doc Link PMC128892 Disease Relevance 1.22 Pain Relevance 0.35
In vitro studies have also demonstrated that viral escape may be a consequence of viral adaptation to the conformational change in CCR5 caused by CCR5 antagonist binding.
CCR5 Binding (binding) of associated with antagonist
14) Confidence 0.34 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.24 Pain Relevance 0.05
Binding of gp120 to the chemokine receptor (either CCR5 or CXCR4) generates a conformational change in gp41, leading to insertion of a lipophilic region of gp41, known as the fusion peptide, into the lipid bilayer of the host cell.
CCR5 Binding (Binding) of associated with chemokine
15) Confidence 0.34 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.49 Pain Relevance 0.13
With its ability to block CCR5 binding and signaling at nanomalor concentrations plus no problematic cytochrome P450 D2 interaction or cardiac ion channel binding, and favorable permeability characteristics, further investigation began of this potent inhibitor of laboratory optimized HIV-1 isolates (mean inhibitory concentration of 90% of isolates or IC90 of 2.0 nM).


CCR5 Binding (binding) of associated with acquired immune deficiency syndrome or hiv infection
16) Confidence 0.34 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2504054 Disease Relevance 0.28 Pain Relevance 0.03
This assay demonstrated that CCR5 occupancy remained at >60% 5 days after discontinuation of maraviroc.
CCR5 Binding (occupancy) of
17) Confidence 0.34 Published 2007 Journal Core Evidence Section Body Doc Link PMC3012555 Disease Relevance 0.17 Pain Relevance 0.05
CCR5 antagonists inhibit virus entry by binding to a host cell protein, the CCR5 receptor, and inducing an allosteric change which renders the molecule unrecognizable to wild type R5 HIV.
CCR5 receptor Binding (binding) of associated with antagonist and acquired immune deficiency syndrome or hiv infection
18) Confidence 0.34 Published 2007 Journal Core Evidence Section Body Doc Link PMC3012555 Disease Relevance 0.71 Pain Relevance 0.20
In-vitro and short-course monotherapy studies suggest that the maraviroc-resistant virus appears to gain the ability to recognize and use the maraviroc-bound CCR5 coreceptor complex (Mosley et al. 2006).
CCR5 coreceptor Binding (recognize) of
19) Confidence 0.34 Published 2007 Journal Core Evidence Section Body Doc Link PMC3012555 Disease Relevance 0.64 Pain Relevance 0.14
Modeling studies demonstrate that the CCR5 antagonists bind in a similar pocket of the CCR5 receptor within the transmembrane region (Westby et al. 2005b).
CCR5 Binding (bind) of associated with antagonist
20) Confidence 0.34 Published 2007 Journal Core Evidence Section Body Doc Link PMC3012555 Disease Relevance 0.23 Pain Relevance 0.10

General Comments

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