Property Summary

NCBI Gene PubMed Count 67
PubMed Score 256.24
PubTator Score 187.38

Knowledge Summary

Patent (17,609)

Expression

Gene RIF (53)

PMID Text
25031337 Infection of CD4+ T cells with HIV-1 in the presence of inhibitors of P2X receptors greatly inhibits HIV-1 infection via both cell-free and cell-to-cell contact in a dose-dependent manner, suggesting P2X receptors interact with gp120/gp41 in viral entry
24845338 These data suggest that vascular smooth muscle cells from human gastro-omental arteries express P2X1 and P2X4 receptor subunits
24661878 With the development of leukemia, the expression of P2X7R increased in both bone marrow and spleen macrophages whereas expression of P2X1 Receptor increased in spleen macrophages.
24633352 enhances platelet activation evoked by mild stimulants via the p38 signalling pathway
23975903 Increased P2X1 receptor expression and ATP release may have contributed to the augmentation of contractile response induced by hypoxia-glucopenia and reoxygenation in he detrusor muscles.
23959888 Data indicate that MgATP2- activates P2X1 and P2X3, but not P2X2 and P2X4 receptors.
23873636 In conclusion, our results demonstrate for the first time that adenine nucleotides acting at P2X1 receptors inhibit the proliferation of human coronary smooth muscle cells via the induction of the early gene NR4A1.
23740251 the contribution of the extracellular, transmembrane, and intracellular segments to recovery from desensitization
22971236 These results suggest that conformational change in the P2X1 receptor is required for co-ordination of ATP action.
22851178 HSP90 inhibitors may be as effective as selective antagonists in regulating platelet P2X1 receptors, and their potential effects on hemostasis should be considered in clinical studies.
22450808 Infection of CD4+ T cells with HIV-1 in the presence of inhibitors of P2X receptors greatly inhibits HIV-1 infection via both cell-free and cell-to-cell contact in a dose-dependent manner, suggesting P2X receptors interact with gp120/gp41 in viral entry
22393010 Agonist binding evokes extensive conformational changes in the extracellular domain of the ATP-gated human P2X1 receptor ion channel
22212928 P2X(1) ion channels play a protective role in endotoxemia by negatively regulating systemic neutrophil activation, thereby limiting the oxidative response, coagulation, and organ damage.
21768526 Studies indicate that P2X1, P2X2, and P2X4 receptors are detected in preglomerular microvessels.
21757694 the cytoskeleton plays an important role in P2X1 receptor regulation
21690089 Cysteine scanning mutagenesis (residues Glu52-Gly96) of the human P2X1 receptor for ATP: mapping agonist binding and channel gating.
20699225 Lipid raft association and cholesterol sensitivity of P2X1-4 receptors for ATP
20660288 T-cell receptor stimulation results in the translocation of P2X1 and P2X4 receptors and pannexin-1 hemichannels to the immune synapse.
20374431 these studies demonstrate for the first time an important role of receptor recycling on P2X1 receptor responsiveness
20345709 PMA-evoked Ca(2+)entry results from an NCX3-dependent dense granule secretion and subsequent P(2X1) receptor activation by secreted ATP, rather than activation of a novel NCCE pathway.
20110693 P2X(1) receptors showed an anti-inflammatory effect reducing NF-kappaB activation and TNF-alpha release.
20068232 Studies indicate that release of ATP and the subsequent activation of P2 receptors help establish the basal level of activation for signal transduction pathways and regulate a wide array of responses.
20024498 TLR2/1 agonist-induced platelet aggregation and secretion depends on a P2X1-mediated Ca2+ mobilisation, production of TxA2 and ADP receptor activation
19808895 Expression is reduced in typ3 2 diabetes, not due to alterations in receptor distribution and mRNA expression, but may be due to differences in receptor sensitivity.
19635923 Activation of P2X1 ion channels by adenosine triphosphate (ATP) promotes neutrophil chemotaxis via Rho kinase-dependent actomyosin-mediated contraction at the cell rear.
19552691 Data confirmed the presence of functional P2X1, P2X4 and P2X7 receptors in LAD2 cells and HLMCs.
19118095 Expression and localization of the nucleotide selective P(2Y2) and P(2X1) receptors suggest that these receptors may mediate ATP-induced vasodilation in skeletal muscle.
18765669 analysis of ectodomain lysines and suramin block of P2X1 receptors
18480058 PAR4-pretreated platelets, epinephrine caused dense granule secretion, and subsequent signaling from the ATP-gated P2X(1)-receptor and the alpha(2A)-adrenergic receptor induced aggregation.
17399929 P2X1 mRNA expression may occur as a result of an increased component of neural ATP release in the aging bladder.
16997281 Co-expression of T18A and K367A mutant P2X1 receptors produced larger ATP evoked responses than either mutant alone and suggests that these amino and carboxy terminal regions interact to regulate channel function
16634759 analysis of a novel interaction between platelet P2X1 and thrombin receptors, with P2X1 functioning to amplify aggregation responses at low levels of thrombin receptor stimulation
16546137 We conclude that lipid rafts play a significant role in the regulation of P2X1 but not P2Y1 receptors in human platelets and that a reserve of non-functional P2X1 receptors may exist.
16529657 identified and characterized the P2X1 promoter utilized in MEG-01 cells and showed that binding of Sp1/3 and NF-1 to elements in the direct vicinity of the transcription start site is essential for basal transcription
16420578 P2X(1) and ERK2 both participate in shear stress controlled thrombosis, but ERK2 activation is initiated predominantly via GPIb-VWF interactions.
16359770 P2X receptor-mediated contractions of human pregnant uterus to alpha,beta-meATP and EFS, but not to ATP, are increased with the progression of pregnancy
16236030 glycine 250 substitution by serine gave functional responses to ATP with no effect on ATP sensitivity but a reduction in peak amplitude to P2X1 receptors
16113781 P2X1 receptors have a role in the early collagen-evoked intracellular Ca2+ responses of human platelets
16006561 Results suggest that lipid rafts play an important role in P2X1 receptor-mediated control of arteries.
15686781 P2X1 receptors are expressed in human cardiomyocytes and mainly distributed in the regions of intercalated discs; there is some close association of P2X1 receptors and connexin43 in some, not all, regions.
15087444 the P2X(1) ion channel induces MLC-mediated cytoskeletal rearrangements, thus contributing to SIPA and degranulation during VWF-triggered platelet activation
14699168 residues Lys-68, Phe-185, Phe-291, Arg-292, and Lys-309 contribute to ligand binding at P2X(1) receptors, with Phe-185 and Phe-291 coordinating the binding of the adenine ring of ATP
14675100 P2X1 stimulation can induce/potentiate platelet activation in combination with other platelet agonists
14557870 Detrusor nerve varicosities from sensory urgency patients revealed general loss of all presynaptic P2X subtypes with the proportion containing receptors reducing to only 0.5-5% depending on P2X subtype.
14500714 the P2X1-ERK2-Myosin Light Chain Kinase axis contributes to collagen-induced platelet activation by enhancing platelet degranulation
12907444 ATP is the principal physiologic agonist at P2X1 receptors and it plays a role in the activation of platelets.
12791671 Decreased expression of the contractile P2X1 receptor could lead to reduced vascular tonus and increased blood flow.
12521992 plays a role in hemostasis and thrombosis through its participation in collagen-, thromboxane A(2)-, and shear stress-triggered platelet responses
12353081 early, transient Ca2+ influx via P2X1 receptors can contribute to platelet activation by stimulating a significant morphological change, but does not readily synergise with P2Y12 receptors to support aggregation
12239162 Mediates activation of extracellular signal-regulated kinase 2 and contributes to platelet secretion and aggregation induced by collagen
12135734 role of tyrosine residues essential for function
11816716 P2X1 ion channel acts as a positive regulator of platelet responses to collagen.
11815371 Ionotropic P2X1 receptors may play a priming role in the subsequent activation of metabotropic P2Y receptors during platelet stimulation.

AA Sequence

MARRFQEELAAFLFEYDTPRMVLVRNKKVGVIFRLIQLVVLVYVIGWVFLYEKGYQTSSGLISSVSVKLK      1 - 70
GLAVTQLPGLGPQVWDVADYVFPAQGDNSFVVMTNFIVTPKQTQGYCAEHPEGGICKEDSGCTPGKAKRK     71 - 140
AQGIRTGKCVAFNDTVKTCEIFGWCPVEVDDDIPRPALLREAENFTLFIKNSISFPRFKVNRRNLVEEVN    141 - 210
AAHMKTCLFHKTLHPLCPVFQLGYVVQESGQNFSTLAEKGGVVGITIDWHCDLDWHVRHCRPIYEFHGLY    211 - 280
EEKNLSPGFNFRFARHFVENGTNYRHLFKVFGIRFDILVDGKAGKFDIIPTMTTIGSGIGIFGVATVLCD    281 - 350
LLLLHILPKRHYYKQKKFKYAEDMGPGAAERDLAATSSTLGLQENMRTS                         351 - 399
//

Text Mined References (67)

PMID Year Title
24845338 2014 Vascular smooth muscle cells from small human omental arteries express P2X1 and P2X4 receptor subunits.
24661878 2014 Functional expression of P2X family receptors in macrophages is affected by microenvironment in mouse T cell acute lymphoblastic leukemia.
24633352 2014 P2X1-initiated p38 signalling enhances thromboxane A2-induced platelet secretion and aggregation.
23975903 2013 Enhanced purinergic contractile responses and P2X1 receptor expression in detrusor muscle during cycles of hypoxia-glucopenia and reoxygenation.
23959888 2013 Subtype-specific control of P2X receptor channel signaling by ATP and Mg2+.
23873636 2013 P2X1 receptor-mediated inhibition of the proliferation of human coronary smooth muscle cells involving the transcription factor NR4A1.
23740251 2013 P2X receptor chimeras highlight roles of the amino terminus to partial agonist efficacy, the carboxyl terminus to recovery from desensitization, and independent regulation of channel transitions.
22971236 2012 Mass spectrometry analysis of human P2X1 receptors; insight into phosphorylation, modelling and conformational changes.
22851178 2012 Heat shock protein 90 inhibitors reduce trafficking of ATP-gated P2X1 receptors and human platelet responsiveness.
22393010 2012 Agonist binding evokes extensive conformational changes in the extracellular domain of the ATP-gated human P2X1 receptor ion channel.
22212928 2012 ATP-gated P2X1 ion channels protect against endotoxemia by dampening neutrophil activation.
21768526 2011 Role of adenosine 5'-triphosphate in regulating renal microvascular function and in hypertension.
21757694 2011 Identification of human P2X1 receptor-interacting proteins reveals a role of the cytoskeleton in receptor regulation.
21690089 2011 Cysteine scanning mutagenesis (residues Glu52-Gly96) of the human P2X1 receptor for ATP: mapping agonist binding and channel gating.
20699225 2010 Lipid raft association and cholesterol sensitivity of P2X1-4 receptors for ATP: chimeras and point mutants identify intracellular amino-terminal residues involved in lipid regulation of P2X1 receptors.
20660288 2010 Pannexin-1 hemichannel-mediated ATP release together with P2X1 and P2X4 receptors regulate T-cell activation at the immune synapse.
20374431 2010 P2X1 receptor mobility and trafficking; regulation by receptor insertion and activation.
20345709 2010 Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry.
20110693 2010 P2X(1) and P2X(3) purinergic receptors differentially modulate the inflammatory response in human osteoarthritic synovial fibroblasts.
20068232 2010 Basal release of ATP: an autocrine-paracrine mechanism for cell regulation.
20024498 2010 Toll-like receptor 2 stimulation of platelets is mediated by purinergic P2X1-dependent Ca2+ mobilisation, cyclooxygenase and purinergic P2Y1 and P2Y12 receptor activation.
19808895 2010 Attenuated purinergic receptor function in patients with type 2 diabetes.
19635923 2009 P2X1 ion channels promote neutrophil chemotaxis through Rho kinase activation.
19552691 2009 Functional evidence for the expression of P2X1, P2X4 and P2X7 receptors in human lung mast cells.
19118095 2009 ATP-induced vasodilation and purinergic receptors in the human leg: roles of nitric oxide, prostaglandins, and adenosine.
18765669 2008 Ectodomain lysines and suramin block of P2X1 receptors.
18480058 2008 The ATP-gated P2X1 receptor plays a pivotal role in activation of aspirin-treated platelets by thrombin and epinephrine.
17895406 2007 Go it alone no more--P2X7 joins the society of heteromeric ATP-gated receptor channels.
17399929 2007 Age-related changes of P2X(1) receptor mRNA in the bladder detrusor from men with and without bladder outlet obstruction.
17207965 2007 hORFeome v3.1: a resource of human open reading frames representing over 10,000 human genes.
16997281 2006 Contribution of P2X1 receptor intracellular basic residues to channel properties.
16634759 2006 P2X1 stimulation promotes thrombin receptor-mediated platelet aggregation.
16546137 2006 Differential sensitivity of human platelet P2X1 and P2Y1 receptors to disruption of lipid rafts.
16529657 2006 Sp1/3 and NF-1 mediate basal transcription of the human P2X1 gene in megakaryoblastic MEG-01 cells.
16420578 2006 ERK2 activation in arteriolar and venular murine thrombosis: platelet receptor GPIb vs. P2X.
16359770 2006 Term-dependency of P2 receptor-mediated contractile responses of isolated human pregnant uterus.
16236030 2005 Contribution of conserved glycine residues to ATP action at human P2X1 receptors: mutagenesis indicates that the glycine at position 250 is important for channel function.
16113781 2005 A major role for P2X1 receptors in the early collagen-evoked intracellular Ca2+ responses of human platelets.
16006561 2005 Disruption of lipid rafts inhibits P2X1 receptor-mediated currents and arterial vasoconstriction.
15686781 2005 P2X1 receptors are closely associated with connexin 43 in human ventricular myocardium.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15313628 2004 Trimeric architecture of homomeric P2X2 and heteromeric P2X1+2 receptor subtypes.
15087444 2004 ATP augments von Willebrand factor-dependent shear-induced platelet aggregation through Ca2+-calmodulin and myosin light chain kinase activation.
14699168 2004 ATP binding at human P2X1 receptors. Contribution of aromatic and basic amino acids revealed using mutagenesis and partial agonists.
14675100 2003 Potentiation of platelet activation through the stimulation of P2X1 receptors.
14557870 2003 Loss of purinergic P2X receptor innervation in human detrusor and subepithelium from adults with sensory urgency.
14500714 2003 P2X1-mediated ERK2 activation amplifies the collagen-induced platelet secretion by enhancing myosin light chain kinase activation.
12907444 2003 Lack of evidence for functional ADP-activated human P2X1 receptors supports a role for ATP during hemostasis and thrombosis.
12791671 2003 Increased mitogenic and decreased contractile P2 receptors in smooth muscle cells by shear stress in human vessels with intact endothelium.
12521992 2003 Overexpression of the platelet P2X1 ion channel in transgenic mice generates a novel prothrombotic phenotype.
12495655 2003 Pharmacological identification of P2X1, P2X4 and P2X7 nucleotide receptors in the smooth muscles of human umbilical cord and chorionic blood vessels.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12353081 2002 Effects of enhanced P2X1 receptor Ca2+ influx on functional responses in human platelets.
12270951 2002 Molecular physiology of P2X receptors.
12239162 2002 P2X(1)-mediated activation of extracellular signal-regulated kinase 2 contributes to platelet secretion and aggregation induced by collagen.
12135734 2002 The intracellular tyrosine residues of the ATP-gated P2X(1) ion channel are essential for its function.
11816716 2001 The ATP-gated P2X1 ion channel acts as a positive regulator of platelet responses to collagen.
11815371 2002 A study of P2X1 receptor function in murine megakaryocytes and human platelets reveals synergy with P2Y receptors.
11809854 2002 Conserved cysteine residues in the extracellular loop of the human P2X(1) receptor form disulfide bonds and are involved in receptor trafficking to the cell surface.
11376948 2001 Regulation of human P2X1 promoter activity by beta helix-loop-helix factors in smooth muscle cells.
10816552 2000 A natural dominant negative P2X1 receptor due to deletion of a single amino acid residue.
10638758 2000 Reduced vas deferens contraction and male infertility in mice lacking P2X1 receptors.
9565569 1998 P2X1 purinoceptor in human platelets. Molecular cloning and functional characterization after heterologous expression.
9558372 1998 The P2X1 receptor, an adenosine triphosphate-gated cation channel, is expressed in human platelets but not in human blood leukocytes.
8834001 1995 Characterization and chromosomal localization of a human P2X receptor from the urinary bladder.
8809107 1996 The human P2x1 receptor: molecular cloning, tissue distribution, and localization to chromosome 17.
2457808 1988 Calcium channels in thrombin-activated human platelet membrane.