INT71758

Context Info Confidence 0.75 First Reported 1997 Last Reported 2010 Negated 3 Speculated 0 Reported most in Body Documents 40 Total Number 54 Disease Relevance 9.01 Pain Relevance 6.14

signal transduction (P2RX1) transport (P2RX1) plasma membrane (P2RX1) protein complex (P2RX1)

Anatomy Link Frequency TM1 4 colon 2 platelets 2 endothelium 2 sensory neurons 1 P2RX1 (Homo sapiens)

Pain Link Frequency Relevance Heat Dorsal horn neuron 7 99.92 dorsal root ganglion 9 99.84 adenocard 191 99.74 antagonist 166 99.22 Neuropeptide 7 99.16 agonist 590 98.92 Glutamate 22 98.40 allodynia 19 97.60 qutenza 6 96.96 cytokine 105 96.68

Disease Link Frequency Relevance Heat Ganglion Cysts 9 99.84 Stress 107 99.54 Diabetes Mellitus 250 99.08 Neuropathic Pain 142 97.60 Apoptosis 19 97.44 Pain 138 96.16 Aids-related Complex 2 94.64 Injury 32 93.04 Nociception 22 91.60 Targeted Disruption 96 88.56

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Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

P2X receptors, a family of ligand-gated ion channels activated by the endogenous ligand ATP, are highly expressed by DRG neurons.

Gene_expression (expressed) of P2X in DRG associated with dorsal root ganglion

1) Confidence 0.75 Published 1997 Journal Nature Section Abstract Doc Link 9338789 Disease Relevance 0.77 Pain Relevance 0.93

This is consistent with a recent report on the cell surface expression of P2X1 receptors (Vacca et al. 2009).

Gene_expression (expression) of P2X1

2) Confidence 0.74 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0.07 Pain Relevance 0

Overall these studies highlight that trafficking plays an important role in the control of the functional expression of P2X1 receptors and their regulation.

Gene_expression (expression) of P2X1

3) Confidence 0.74 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0 Pain Relevance 0.11

HEK293 cells stably expressing P2X1-4 receptors were used to determine whether these receptors were localized in lipid rafts.

Gene_expression (expressing) of P2X1

4) Confidence 0.72 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0.04

The P2X1 receptor was detected in the same fractions as flotillin as we have shown previously (10).

Gene_expression (detected) of P2X1 receptor

5) Confidence 0.72 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0.04

Cell surface expression of the P2X1 receptor was also unaffected by cholesterol disruption (Fig. 3a, lower panel) demonstrating that a change in receptor number does not account for the inhibition of P2X1 receptor responses.

Gene_expression (expression) of P2X1 receptor

6) Confidence 0.72 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0.09

Microglia also express another subtype of P2XR, P2X7R, but this receptor subtype appears not to be involved because activation of P2X7Rs typically requires a higher concentration of ATP than used [76, 77] and because TNP-ATP, which does not affect P2X7Rs [78], prevents ATP from stimulating microglia to produce allodynia.

Gene_expression (express) of P2XR in microglia associated with allodynia

7) Confidence 0.65 Published 2005 Journal Purinergic Signal Section Body Doc Link PMC2096535 Disease Relevance 1.14 Pain Relevance 0.92

The limited contribution of newly synthesised P2X1 receptors to FRAP suggests that recovery results predominantly from lateral diffusion of receptors already at the cell surface and/or the insertion of recycling receptors.

Gene_expression (synthesised) of P2X1 in lateral

8) Confidence 0.64 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0 Pain Relevance 0.03

Does receptor recycling contribute to P2X1 receptors FRAP?

Gene_expression (receptors) of P2X1

9) Confidence 0.64 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0 Pain Relevance 0.03

The increase in time constant of recovery of P2X1 FRAP following phorbol ester treatment is consistent with a decrease in the time required for recovery from desensitisation (Ase et al. 2005).

Gene_expression (recovery) of P2X1 FRAP

10) Confidence 0.64 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0 Pain Relevance 0.13

The modest effects of the protein synthesis inhibitor cycloheximide on FRAP suggest that insertion of newly synthesised P2X1 receptors at the cell surface makes only a small contribution to recovery from photo-bleaching.

Gene_expression (synthesised) of P2X1

11) Confidence 0.64 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0.06 Pain Relevance 0

P2X1-eGFP receptor fluorescence recovered with a time constant of ?

Gene_expression (recovered) of P2X1

12) Confidence 0.64 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0 Pain Relevance 0

A characteristic feature of P2X1 receptors is that they show rapid receptor desensitisation (time constant ?

Gene_expression (receptors) of P2X1

13) Confidence 0.64 Published 2010 Journal Journal of Neurochemistry Section Body Doc Link PMC2878604 Disease Relevance 0 Pain Relevance 0.05

Swapping the P2X2 receptor TM1 (P2X1-2b), extracellular domain (P2X1-2c), or second half of the carboxyl terminus (P2X1-2e?)

Gene_expression (Swapping) of P2X1-2c in TM1

14) Confidence 0.63 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0

To characterize further the contribution of the amino terminus of the P2X1 receptor to cholesterol sensitivity, two additional chimeras were generated, P2X1-2a?

Gene_expression (generated) of P2X1-2a

15) Confidence 0.63 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0

for the equivalent P2X1 receptor region reduced the effects of cholesterol depletion by ?

Gene_expression (region) of P2X1 receptor

16) Confidence 0.63 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0

Swapping the P2X2 receptor TM1 (P2X1-2b), extracellular domain (P2X1-2c), or second half of the carboxyl terminus (P2X1-2e?)

Gene_expression (Swapping) of P2X1 in TM1

17) Confidence 0.63 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0

Alternatively, the cells expressing P2X1-4 subtype receptors were lysed in 2 ml of MBS (25 mm MES and 150 mm NaCl, pH 6.5) containing Triton X-100 (0.1, 0.3, or 1%).

Gene_expression (expressing) of P2X1

18) Confidence 0.63 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0

Swapping the P2X2 receptor TM1 (P2X1-2b), extracellular domain (P2X1-2c), or second half of the carboxyl terminus (P2X1-2e?)

Gene_expression (Swapping) of P2X2 receptor TM1 in TM1

19) Confidence 0.63 Published 2010 Journal The Journal of Biological Chemistry Section Body Doc Link PMC2963349 Disease Relevance 0 Pain Relevance 0

HEK293 cells stably expressing the P2X1 receptor were treated with 1 ?

Gene_expression (expressing) of P2X1 receptor

20) Confidence 0.60 Published 2009 Journal Neuropharmacology Section Body Doc Link PMC2613953 Disease Relevance 0 Pain Relevance 0.03

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