P2Y12

Summary

Gene Symbol: P2Y12
Description: purinergic receptor P2Y12
Alias: ADPG-R, BDPLT8, HORK3, P2T(AC), P2Y(12)R, P2Y(AC), P2Y(ADP), P2Y(cyc), P2Y12, SP1999, P2Y purinoceptor 12, ADP-glucose receptor, G-protein coupled receptor SP1999, Gi-coupled ADP receptor HORK3, P2Y12 platelet ADP receptor, purinergic receptor P2RY12, purinergic receptor P2Y, G-protein coupled, 12
Species: human

Top Publications

  1. ncbi Novel molecular defect in the platelet ADP receptor P2Y12 of a patient with haemorrhagic diathesis
    Jasper A Remijn
    Department of Clinical Chemistry and Laboratory Medicine, Isala Klinieken, Zwolle, The Netherlands
    Clin Chem Lab Med 45:187-9. 2007
  2. ncbi Assessment of clopidogrel responsiveness: measurements of maximum platelet aggregation, final platelet aggregation and their correlation with vasodilator-stimulated phosphoprotein in resistant patients
    Paul A Gurbel
    Sinai Center for Thrombosis Research, Baltimore, Maryland 21215, USA
    Thromb Res 121:107-15. 2007
  3. ncbi Frontiers in platelet inhibition
    David Varon
    Coagulation Unit, Hadassah Hebrew University Medical Center, Jerusalem, Israel
    Discov Med 8:242-6. 2009
  4. doi Comparison of platelet function tests in predicting clinical outcome in patients undergoing coronary stent implantation
    Nicoline J Breet
    Department of Cardiology, St Antonius Hospital, PO Box 2500, 3435 CM Nieuwegein, The Netherlands
    JAMA 303:754-62. 2010
  5. doi Role of phosphoinositide 3-kinase beta in platelet aggregation and thromboxane A2 generation mediated by Gi signalling pathways
    Analia Garcia
    Department of Physiology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Biochem J 429:369-77. 2010
  6. ncbi Purinergic P2Y12 receptor blockade inhibits shear-induced platelet phosphatidylinositol 3-kinase activation
    Julio C Reséndiz
    VA Medical Center, Baylor College of Medicine, Texas, USA
    Mol Pharmacol 63:639-45. 2003
  7. ncbi ADP is the cognate ligand for the orphan G protein-coupled receptor SP1999
    F L Zhang
    Human Genome Research, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    J Biol Chem 276:8608-15. 2001
  8. ncbi Identification of the platelet ADP receptor targeted by antithrombotic drugs
    G Hollopeter
    Department of Cellular and Molecular Pharmacology, University of California, San Francisco 94143, USA
    Nature 409:202-7. 2001
  9. ncbi Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor
    J Takasaki
    Molecular Medicine Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co, Ltd, Ibaraki, Japan
    Mol Pharmacol 60:432-9. 2001
  10. pmc Molecular bases of defective signal transduction in the platelet P2Y12 receptor of a patient with congenital bleeding
    Marco Cattaneo
    A Bianchi Bonomi Hemophilia and Thrombosis Center, Department of Internal Medicine, Istituto di Ricovero e Cura a Carattere Scientifico Ospedale Maggiore, University of Milan, 20122 Milan, Italy
    Proc Natl Acad Sci U S A 100:1978-83. 2003

Research Grants

  1. Novel Antithrombotic Diadenosine Tetraphosphate Analogs
    IVAN B YANACHKOV; Fiscal Year: 2010
  2. IVAN B YANACHKOV; Fiscal Year: 2015
  3. Michael R King; Fiscal Year: 2014
  4. Role of Beta 3 Integrin in Skeletal Metastasis
    Katherine Weilbaecher; Fiscal Year: 2009
  5. Antiplatelet Therapy: Platelet Inhibition, Polymorphisms, and Protein Biomarkers
    Marc S Sabatine; Fiscal Year: 2012
  6. BLOOD PLATELET THROMBOXANE RECEPTORS
    GUY C LEBRETON; Fiscal Year: 2013
  7. Novel Molecules in Calcium Signaling in Platelets
    Wolfgang Bergmeier; Fiscal Year: 2013
  8. Joshua A Boyce; Fiscal Year: 2016
  9. KATHERINE NELSON WEILBAECHER; Fiscal Year: 2014
  10. P2T PURINERGIC RECEPTORS
    JOSE BOYER; Fiscal Year: 2004

Detail Information

Publications217 found, 100 shown here

  1. ncbi Novel molecular defect in the platelet ADP receptor P2Y12 of a patient with haemorrhagic diathesis
    Jasper A Remijn
    Department of Clinical Chemistry and Laboratory Medicine, Isala Klinieken, Zwolle, The Netherlands
    Clin Chem Lab Med 45:187-9. 2007
    ..We report a novel molecular defect in the gene coding for P2Y(12) in a patient with a history of epistaxis, easy bruising and excessive posttraumatic blood loss...
  2. ncbi Assessment of clopidogrel responsiveness: measurements of maximum platelet aggregation, final platelet aggregation and their correlation with vasodilator-stimulated phosphoprotein in resistant patients
    Paul A Gurbel
    Sinai Center for Thrombosis Research, Baltimore, Maryland 21215, USA
    Thromb Res 121:107-15. 2007
    Controversy surrounds the optimal platelet aggregation measurement to assess clopidogrel non-responsiveness. The P2Y12 reactivity ratio (PRR) determined by vasodilator-stimulated phosphoprotein phosphorylation levels has been used to ..
  3. ncbi Frontiers in platelet inhibition
    David Varon
    Coagulation Unit, Hadassah Hebrew University Medical Center, Jerusalem, Israel
    Discov Med 8:242-6. 2009
    ..After many years of a "monopoly" of aspirin, ADP receptor P2Y12 inhibitors were introduced with a significant improvement in clinical outcome...
  4. doi Comparison of platelet function tests in predicting clinical outcome in patients undergoing coronary stent implantation
    Nicoline J Breet
    Department of Cardiology, St Antonius Hospital, PO Box 2500, 3435 CM Nieuwegein, The Netherlands
    JAMA 303:754-62. 2010
    ..On-treatment platelet reactivity was measured in parallel by light transmittance aggregometry, Verify Now P2Y12 and Platelet works assays, and the IMPACT-R and the platelet function analysis system (PFA-100) (with the Dade PFA ..
  5. doi Role of phosphoinositide 3-kinase beta in platelet aggregation and thromboxane A2 generation mediated by Gi signalling pathways
    Analia Garcia
    Department of Physiology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Biochem J 429:369-77. 2010
    PI3Ks (phosphoinositide 3-kinases) play a critical role in platelet functional responses. PI3Ks are activated upon P2Y12 receptor stimulation and generate pro-aggregatory signals...
  6. ncbi Purinergic P2Y12 receptor blockade inhibits shear-induced platelet phosphatidylinositol 3-kinase activation
    Julio C Reséndiz
    VA Medical Center, Baylor College of Medicine, Texas, USA
    Mol Pharmacol 63:639-45. 2003
    ..PI3-K activation is signaled by rapid feedback amplification that involves P2Y(12) receptor-mediated activation of Syk...
  7. ncbi ADP is the cognate ligand for the orphan G protein-coupled receptor SP1999
    F L Zhang
    Human Genome Research, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    J Biol Chem 276:8608-15. 2001
    ..Additional ADP receptors linked to Galpha(i) have been described but have not yet been cloned. SP1999 is an orphan G protein-coupled receptor, which is highly expressed in brain, spinal cord, and blood platelets...
  8. ncbi Identification of the platelet ADP receptor targeted by antithrombotic drugs
    G Hollopeter
    Department of Cellular and Molecular Pharmacology, University of California, San Francisco 94143, USA
    Nature 409:202-7. 2001
    ..9). Here we describe the cloning of this receptor, designated P2Y12, and provide evidence that a patient with a bleeding disorder has a defect in this gene...
  9. ncbi Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor
    J Takasaki
    Molecular Medicine Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co, Ltd, Ibaraki, Japan
    Mol Pharmacol 60:432-9. 2001
    ..The cDNA encoding a novel G protein-coupled receptor, termed HORK3, was isolated. The HORK3 gene and P2Y(1) gene were mapped to chromosome 3q21-q25...
  10. pmc Molecular bases of defective signal transduction in the platelet P2Y12 receptor of a patient with congenital bleeding
    Marco Cattaneo
    A Bianchi Bonomi Hemophilia and Thrombosis Center, Department of Internal Medicine, Istituto di Ricovero e Cura a Carattere Scientifico Ospedale Maggiore, University of Milan, 20122 Milan, Italy
    Proc Natl Acad Sci U S A 100:1978-83. 2003
    ..These studies delineate a region of P2Y(12) required for normal function after ADP binding...
  11. ncbi P2Y12 H2 haplotype is associated with peripheral arterial disease: a case-control study
    Pierre Fontana
    INSERM U 428, Hôpital Européen Georges Pompidou et Université Paris V, Paris, France
    Circulation 108:2971-3. 2003
    We recently described a gain-of-function haplotype, called H2, of the adenosine diphosphate (ADP) receptor P2Y12 gene associated with increased ADP-induced platelet aggregation ex vivo in healthy volunteers...
  12. ncbi Dimorphism in the P2Y1 ADP receptor gene is associated with increased platelet activation response to ADP
    Simon L Hetherington
    Department of Cardiovascular Sciences, University of Leicester, United Kingdom
    Arterioscler Thromb Vasc Biol 25:252-7. 2005
    The platelet ADP receptors P2Y1 and P2Y12 play a pivotal role in platelet aggregation. There is marked interindividual variation in platelet response to ADP...
  13. ncbi P2Y12 gene H2 haplotype is not associated with increased adenosine diphosphate-induced platelet aggregation after initiation of clopidogrel therapy with a high loading dose
    Nicolas von Beckerath
    Deutsches Herzzentrum, Technische Universitat Munchen, Lazarettstrasse 36, 80636 Munich, Germany
    Blood Coagul Fibrinolysis 16:199-204. 2005
    A large variability in the antiplatelet response to clopidogrel has been consistently reported. Recently, a P2Y12 haplotype was shown to be associated with enhanced adenosine diphosphate (ADP)-induced platelet aggregation in healthy ..
  14. ncbi Association of a functional polymorphism in the clopidogrel target receptor gene, P2Y12, and the risk for ischemic cerebrovascular events in patients with peripheral artery disease
    Sophie Ziegler
    Department of Internal Medicine II, Vienna General Hospital, Medical University of Vienna, Austria
    Stroke 36:1394-9. 2005
    ..We tested for an association of gene sequence variations in P2Y12 and occurrence of neurological adverse events in patients with symptomatic peripheral artery disease (PAD) during ..
  15. ncbi Lack of association between the P2Y12 receptor gene polymorphism and platelet response to clopidogrel in patients with coronary artery disease
    Dominick J Angiolillo
    Division of Cardiology, University of Florida Shands Jacksonville, 655 West 8th Street, Jacksonville, FL 32209, USA
    Thromb Res 116:491-7. 2005
    ..However, the role of gene sequence variations of the P2Y(12) receptor in patients treated with clopidogrel has not yet been assessed...
  16. ncbi Association between platelet P2Y12 haplotype and risk of cardiovascular events in chronic coronary disease
    Isolmar T Schettert
    Heart Institute, University of Sao Paulo Medical School, Sao Paulo, Brazil
    Thromb Res 118:679-83. 2006
    A positive association was recently described between P2Y12 platelet receptor H1 and H2 haplotypes and peripheral artery disease. We tested the described P2Y12 receptor haplotypes in a group of patients with coronary artery disease.
  17. ncbi Genetic polymorphisms of the platelet receptors P2Y(12), P2Y(1) and GP IIIa and response to aspirin and clopidogrel
    Eli I Lev
    The Methodist DeBakey Heart Center, The Methodist Hospital and Baylor College of Medicine, Section of Cardiology, 6565 Fannin St Mail Station F 1090, Houston, TX 77030, USA
    Thromb Res 119:355-60. 2007
    ..Polymorphisms of several platelet receptors have been related to increased platelet aggregation. We therefore aimed to evaluate whether these polymorphisms are related to altered response to aspirin or clopidogrel...
  18. ncbi Common sequence variations in the P2Y12 and CYP3A5 genes do not explain the variability in the inhibitory effects of clopidogrel therapy
    Simon M G Smith
    Cardiovascular Research Unit, University of Sheffield, Division of Clinical Sciences North, Northern General Hospital, Sheffield, UK
    Platelets 17:250-8. 2006
    The efficacy of the platelet P2Y12 receptor antagonist clopidogrel, which undergoes cytochrome-mediated metabolism to its active form, shows marked inter-individual variability...
  19. ncbi Continuous signaling via PI3K isoforms beta and gamma is required for platelet ADP receptor function in dynamic thrombus stabilization
    Judith M E M Cosemans
    Department of Biochemistry and Human Biology, Cardiovascular Research Institute Maastricht CARIM, University of Maastricht, PO Box 616, 6200 MD Maastricht, The Netherlands
    Blood 108:3045-52. 2006
    ..1) in the absence of fibrinogen-containing plasma; (2) by blocking or inhibiting alpha(IIb)beta3; (3) by blocking P2Y12 receptors; (4) by suppression of phosphoinositide 3-kinase (PI3K) beta...
  20. ncbi Role of the T744C polymorphism of the P2Y12 gene on platelet response to a 600-mg loading dose of clopidogrel in 597 patients with non-ST-segment elevation acute coronary syndrome
    Thomas Cuisset
    Department of Cardiology, CHU Timone, Marseille, France
    Thromb Res 120:893-9. 2007
    ..However, the underlying mechanisms remain unclear. Recently, the T744C polymorphism of the P2Y12 receptor gene has been associated with enhanced platelet aggregation in healthy volunteers, suggesting a possible ..
  21. pmc Gene sequence variations of the platelet P2Y12 receptor are associated with coronary artery disease
    Ugo Cavallari
    Department of Mother and Child and of Biology Genetics, Section of Biology and Genetics, University of Verona, Verona, Italy
    BMC Med Genet 8:59. 2007
    The platelet P2Y12 receptor plays a key role in platelet activation...
  22. ncbi Coexisting polymorphisms of P2Y12 and CYP2C19 genes as a risk factor for persistent platelet activation with clopidogrel
    Lukasz A Malek
    Coronary Disease Department and II Catheterization Laboratory, Institute of Cardiology, Alpejska 42 str, 04 628 Warsaw, Poland
    Circ J 72:1165-9. 2008
    ..Coexisting polymorphisms of the genes affecting clopiogrel resistance may influence platelet activation...
  23. pmc The Gi-coupled P2Y12 receptor regulates diacylglycerol-mediated signaling in human platelets
    Gianni F Guidetti
    Center of Excellence for Applied Biology, Department of Biochemistry, University of Pavia, via Bassi 21, 27100 Pavia, Italy
    J Biol Chem 283:28795-805. 2008
    ..inhibited not only by an antagonist of the G(q)-coupled P2Y1 receptor but also upon blockade of the G(i)-coupled P2Y12 receptor...
  24. ncbi Functional variability of platelet response to clopidogrel correlates with P2Y(12) receptor occupancy
    Claire Bal dit Sollier
    IVS, Hopital Lariboisiere, Paris, France
    Thromb Haemost 101:116-22. 2009
    ..An additional 300 mg dose of clopidogrel improves both IPA and P2Y(12) receptor occupancy mostly in the subset of 'low' responders...
  25. doi Identification and characterization of a novel P2Y 12 variant in a patient diagnosed with type 1 von Willebrand disease in the European MCMDM-1VWD study
    Martina E Daly
    Academic Unit of Haematology, School of Medicine and Biomedical Sciences, University of Sheffield, Sheffield, United Kingdom
    Blood 113:4110-3. 2009
    ..Our results provide further evidence for locus heterogeneity in type 1 VWD...
  26. doi The platelet P2Y₁₂ receptor for adenosine diphosphate: congenital and drug-induced defects
    Marco Cattaneo
    Unità di Medicina 3, Ospedale San Paolo, Dipartimento di Medicina, Chirurgia e Odontoiatria, Universita degli Studi di Milano, Milano, Italy
    Blood 117:2102-12. 2011
    ..Although they increase the incidence of major bleedings, the net clinical benefit is in favor of the new P2Y₁₂ inhibitors...
  27. doi The extent of P2Y12 inhibition by clopidogrel in diabetes mellitus patients with acute coronary syndrome is not related to glycaemic control: roles of white blood cell count and body weight
    Olivier Morel
    Pôle d activité médico chirurgicale Cardiovasculaire, Nouvel Hopital Civil, Universite de Strasbourg, France
    Thromb Haemost 108:338-48. 2012
    ..In this study, the extent of P2Y12 ADP receptor pathway inhibition was evaluated by the VASP-FCT...
  28. ncbi Adenosine diphosphate-induced platelet aggregation is associated with P2Y12 gene sequence variations in healthy subjects
    Pierre Fontana
    Service d Hématologie Biologique A, Hôpital Européen Georges Pompidou and Inserm Unité 428, Faculte des Sciences Pharmaceutiques et Biologiques, Universite Paris V, Paris, France
    Circulation 108:989-95. 2003
    The adenosine diphosphate (ADP) receptor P2Y12 plays a pivotal role in platelet aggregation, as demonstrated by the benefit conferred by its blockade in patients with cardiovascular disease...
  29. ncbi Identification of endogenous surrogate ligands for human P2Y12 receptors by in silico and in vitro methods
    Yosuke Nonaka
    Laboratory of Pharmcoinformatics, Department of Bioinformatics, Ritsumeikan University, Kusatsu, Shiga 525 8577, Japan
    Biochem Biophys Res Commun 337:281-8. 2005
    Endogenous ligands acting on a human P2Y12 receptor, one of the G-protein coupled receptors, were searched by in silico screening against our own database, which contains more than 500 animal metabolites...
  30. doi [The basis of platelets: platelets and atherothrombosis: an understanding of the lack of efficacy of aspirin in peripheral arterial disease (PAD) and diabetic patients]
    Ludovic Drouet
    Haematology Laboratory, Lariboisiere University Hospital, Paris, France
    Drugs 70:9-14. 2010
    ..thienopyridines suppress the platelet aggregation adenosine diphosphate (ADP) pathway by inhibiting the platelet P2Y12 subtype of the ADP receptor...
  31. ncbi Platelet P2 receptors: old and new targets for antithrombotic drugs
    Marco Cattaneo
    Universita degli Studi di Milano, Unità di Ematologia e Trombosi Ospedale San Paolo, Via di Rudinì 820142 Milano, Italy
    Expert Rev Cardiovasc Ther 5:45-55. 2007
    Platelets possess three P2 receptors for adenine nucleotides: P2Y1 and P2Y12, which interact with ADP, and P2X1, which interacts with ATP...
  32. ncbi The P2Y12 receptor as a therapeutic target in cardiovascular disease
    R F Storey
    Cardiovascular Medicine, University Hospital, Queen s Medical Centre, Nottingham, NG7 2UH, UK
    Platelets 12:197-209. 2001
    ..Orally active ATP analogues are also being developed that may be more effective than clopidogrel. Limitations of platelet glycoprotein IIb/IIIa antagonists leave scope for development of alternative antiplatelet agents...
  33. pmc A multiple dose study of prasugrel (CS-747), a novel thienopyridine P2Y12 inhibitor, compared with clopidogrel in healthy humans
    Joseph A Jakubowski
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Br J Clin Pharmacol 63:421-30. 2007
    ....
  34. ncbi Ticlopidine pretreatment before coronary stenting is associated with sustained decrease in adverse cardiac events: data from the Evaluation of Platelet IIb/IIIa Inhibitor for Stenting (EPISTENT) Trial
    S R Steinhubl
    Department of Cardiology, Wilford Hall Medical Center, Lackland AFB, TX 78236, USA
    Circulation 103:1403-9. 2001
    ..The role of enhanced antiplatelet protection through pretreatment with the platelet ADP-receptor antagonist ticlopidine in preventing both the early and late complications of coronary stenting has not previously been explored...
  35. ncbi Platelet ADP receptor antagonists: ticlopidine and clopidogrel
    Alan K Jacobson
    Research Service 151, Loma Linda VA Medical Center, 11201 Benton Street, Loma Linda, CA 92354, USA
    Best Pract Res Clin Haematol 17:55-64. 2004
    ..The action of clopidogrel is similar to that of ticlopidine, and it is comparably effective. However, the side-effect profile of clopidogrel is much more favorable...
  36. pmc Gi- and Gq-coupled ADP (P2Y) receptors act in opposition to modulate nociceptive signaling and inflammatory pain behavior
    Sacha A Malin
    Dept Medicine Dept Neurobiology, University of Pittsburgh, Pittsburgh, PA, USA
    Mol Pain 6:21. 2010
    ..In this study, we examined the expression and function of P2Y1 and the Gi-coupled receptors P2Y12, P2Y13 and P2Y14 in sensory neurons to determine their contribution to nociception.
  37. ncbi A comparison of prasugrel and clopidogrel loading doses on platelet function: magnitude of platelet inhibition is related to active metabolite formation
    John T Brandt
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Am Heart J 153:66.e9-16. 2007
    ..Thienopyridines are prodrugs, metabolized in vivo to active metabolites that inhibit the platelet P2Y12 adenosine diphosphate (ADP) receptor.
  38. ncbi The significance of vasodilator-stimulated phosphoprotein for risk stratification of stent thrombosis
    Rüdiger Blindt
    Department of Cardiology, University Hospital Aachen, Pauwelsstr 30, 52074 Aachen, Germany
    Thromb Haemost 98:1329-34. 2007
    Low-response to the P2Y12 adenosine diphosphate (ADP)-receptor antagonist clopidogrel was suggested to correspond to a higher incidence of stent thrombosis (ST)...
  39. pmc Systemic low-dose aspirin and clopidogrel independently attenuate reflex cutaneous vasodilation in middle-aged humans
    Lacy A Holowatz
    Department of Kinesiology, The Pennsylvania State University, 113 Noll Lab, Univ Park, PA 16802, USA
    J Appl Physiol (1985) 108:1575-81. 2010
    ..001). ASA-induced COX and specific platelet ADP receptor inhibition attenuate reflex vasodilation, suggesting platelet involvement in reflex vasodilation through the release of vasodilating factors...
  40. ncbi Inhibitory purinergic transmission in mouse caecum: role for P2Y1 receptors as prejunctional modulators of ATP release
    M G Zizzo
    Dipartimento di Biologia Cellulare e dello Sviluppo, Universita di Palermo, Viale delle Scienze, 90128 Palermo, Italy
    Neuroscience 150:658-64. 2007
    ..acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethyl-propionyl-oxymethyl)-propyl ester (MRS 2395), P2Y11 and P2Y12 purinoceptor antagonist, were without any effect...
  41. ncbi Platelet collagen receptor integrin alpha2beta1 activation involves differential participation of ADP-receptor subtypes P2Y1 and P2Y12 but not intracellular calcium change
    S M Jung
    Department of Protein Biochemistry, Institute of Life Science, Kurume University, Japan
    Eur J Biochem 268:3513-22. 2001
    ..and their relative contributions to alpha2beta1 activation (assessed by soluble-collagen binding) using the P2Y12 antagonist AR-C69931MX and P2Y1 antagonists adenosine 3',5'-diphosphate (Ado(3,5)PP) and adenosine 3'-phosphate 5'-..
  42. pmc Roles and interactions among protease-activated receptors and P2ry12 in hemostasis and thrombosis
    Ivo Cornelissen
    Cardiovascular Research Institute, University of California, San Francisco, CA 94158, USA
    Proc Natl Acad Sci U S A 107:18605-10. 2010
    ..These results make predictions being tested by ongoing human trials and suggest hypotheses for new antithrombotic strategies...
  43. ncbi Regulated expression of active biotinylated G-protein coupled receptors in mammalian cells
    Gregory J Mize
    Department of Urology, University of Washington, Seattle, WA 98195, USA
    Protein Expr Purif 57:280-9. 2008
    ....
  44. pmc Regulation and functional consequences of ADP receptor-mediated ERK2 activation in platelets
    Analia Garcia
    Department of Physiology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Biochem J 404:299-308. 2007
    ..G(q)-coupled P2Y1 receptor (platelet ADP receptor coupled to stimulation of phospholipase C) and the G(i)-coupled P2Y12 receptor (platelet ADP receptor coupled to inhibition of adenylate cyclase) in addition to outside-in signalling...
  45. ncbi Gi-coupled P2Y-ADP receptor mediates GSK-3 phosphorylation and beta-catenin nuclear translocation in granule neurons
    Felipe Ortega
    Department of Biochemistry, Veterinary Faculty, Complutense University of Madrid, Madrid, Spain
    J Neurochem 104:62-73. 2008
    ..The present study first describes the coupling of a Gi-coupled P2Y(13)-like receptor to GSK-3 and beta-catenin through PI3-K/Akt signaling...
  46. doi P2Y12 receptor upregulation in activated microglia is a gateway of p38 signaling and neuropathic pain
    Kimiko Kobayashi
    Department of Anatomy and Neuroscience, Hyogo College of Medicine, Nishinomiya, Hyogo 663 8501, Japan
    J Neurosci 28:2892-902. 2008
    ..Activation of this receptor by released ATP or the hydrolyzed products activate p38 MAPK pathway and may play a crucial role in the generation of neuropathic pain...
  47. doi Attenuation of transplant arteriosclerosis with clopidogrel is associated with a reduction of infiltrating dendritic cells and macrophages in murine aortic allografts
    Silke Abele
    Department of Cardiac Surgery, Friedrich Alexander University Erlangen Nurnberg, Germany
    Transplantation 87:207-16. 2009
    ..Monotherapy with clopidogrel reduced the formation of transplant arteriosclerosis in a murine aortic allograft model. However, the underlying immunologic mechanisms are still unknown...
  48. doi Shear-induced global thrombosis test of native blood: pivotal role of ADP allows monitoring of P2Y12 antagonist therapy
    S Saraf
    Cardiology Department, East and North Hertfordshire NHS Trust, Welwyn Garden City, Hertfordshire, United Kingdom
    Thromb Res 124:447-51. 2009
    ..However, the fact that red blood cells (RBC) are essential to achieve platelet aggregation in these tests supports recent evidence that ADP makes an important contribution to shear-induced platelet reaction...
  49. doi Emerging oral antiplatelet therapies for acute coronary syndromes
    Charles V Pollack
    Department of Emergency Medicine, Pennsylvania Hospital, Philadelphia, PA 19107, USA
    Hosp Pract (1995) 38:29-37. 2010
    ..The current standard-of-care oral antiplatelet therapy for ACS is aspirin in combination with a P2Y12 adenosine diphosphate (ADP) receptor antagonist, most commonly clopidogrel...
  50. pmc Molecular identification and characterization of the platelet ADP receptor targeted by thienopyridine antithrombotic drugs
    C J Foster
    Department of Central Nervous System and Cardiovascular Pharmacology, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    J Clin Invest 107:1591-8. 2001
    ..Recently, we cloned a human orphan receptor, SP1999, highly expressed in brain and platelets, which responded to ADP and had a pharmacological profile similar to that ..
  51. doi Safety and feasibility of adjunctive antiplatelet therapy with intravenous elinogrel, a direct-acting and reversible P2Y12 ADP-receptor antagonist, before primary percutaneous intervention in patients with ST-elevation myocardial infarction: the Early Rap
    Jeffrey S Berger
    Duke Clinical Research Institute, Duke University Medical Center, Durham, NC 27705, USA
    Am Heart J 158:998-1004.e1. 2009
    Inhibition of the P2Y12 ADP-receptor with oral antiplatelet agents given to patients undergoing primary percutaneous coronary intervention (PCI) for ST-elevation myocardial infarction (STEMI) is associated with improved outcomes, but ..
  52. doi Comparison of conventional aggregometry with VASP for monitoring P2Y12-specific platelet inhibition
    Daniel Aradi
    Department of Interventional Cardiology, Heart Institute, University of Pecs, Hungary
    Platelets 21:563-70. 2010
    No consensus exists regarding the optimal estimate of light transmission aggregometry (LTA) to reflect P2Y12 ADP receptor inhibition in patients receiving thienopyridine therapy...
  53. ncbi P2Y12, a new platelet ADP receptor, target of clopidogrel
    Jean Marc Herbert
    Sanofi Synthelabo Recherche, Toulouse, France
    Semin Vasc Med 3:113-22. 2003
    ..Another Gi (2)-coupled receptor (named P2Y12) has been recently cloned and stably expressed in CHO cells...
  54. ncbi Variable extent of clopidogrel responsiveness in patients after coronary stenting
    Ralf Grossmann
    Central Laboratory and Blood Coagulation Unit, Institute of Clinical Biochemistry and Pathobiochemistry, University of Wurzburg, Josef Schneider Str 2, 97080 Wurzburg, Germany
    Thromb Haemost 92:1201-6. 2004
    ..After metabolic activation, the active clopidogrel metabolite irreversibly impairs the human platelet P2Y12 ADP receptor...
  55. ncbi Evidence for two distinct G-protein-coupled ADP receptors mediating platelet activation
    H M Jantzen
    COR Therapeutics, Inc, South San Francisco, CA 94080, USA
    Thromb Haemost 81:111-7. 1999
    ....
  56. ncbi Platelets from a patient heterozygous for the defect of P2CYC receptors for ADP have a secretion defect despite normal thromboxane A2 production and normal granule stores: further evidence that some cases of platelet 'primary secretion defect' are heteroz
    M Cattaneo
    Angelo Bianchi Bonomi Hemophilia and Thrombosis Center, Department of Internal Medicine IRCCS Ospedale Maggiore, University of Milan, Milan, Italy
    Arterioscler Thromb Vasc Biol 20:E101-6. 2000
    ....
  57. ncbi Activation of Rap1B by G(i) family members in platelets
    Donna Woulfe
    Department of Medicine, Center for Experimental Therapeutics, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Biol Chem 277:23382-90. 2002
    ..We also show that platelets from mice lacking G(alpha)(i2), which couples to the ADP receptor, P2Y12, exhibit reduced Rap1 activation in response to ADP...
  58. ncbi Comparison of the pharmacodynamic effects of the platelet ADP receptor antagonists clopidogrel and AR-C69931MX in patients with ischaemic heart disease
    Robert F Storey
    Cardiovascular Medicine, University Hospital, Queen s Medical Centre, Nottingham, NG7 2UH, UK
    Platelets 13:407-13. 2002
    ..In conclusion, therapeutic administration of clopidogrel moderately inhibits platelet P2Y(12) receptor activation and substantially greater P2Y(12) receptor blockade can be achieved with AR-C69931MX...
  59. ncbi Quantification of ADP and ATP receptor expression in human platelets
    L Wang
    Department of Cardiology, Lund University Hospital, Lund, Sweden
    J Thromb Haemost 1:330-6. 2003
    ..In platelets from healthy volunteers, only P2X1, P2Y1 and P2Y12 were found in significant levels, with the following order of expression: P2Y12 >> P2X1 > P2Y1...
  60. ncbi Platelet ADP receptors contribute to the initiation of intravascular coagulation
    Catherine Leon
    Institut fur Klinische Chemie, Ludwig Maximilians Universitat Munchen, Marchioninistr 15, 81377 Munchen, Germany
    Blood 103:594-600. 2004
    ..Ex vivo inhibition of the P2Y12 ADP receptor by clopidogrel administration diminished the rapid exposure of tissue factor (TF), the major ..
  61. ncbi Pharmacokinetics of clopidogrel after administration of a high loading dose
    Dirk Taubert
    Department of Pharmacology, University Hospital, University of Cologne, Cologne, Germany
    Thromb Haemost 92:311-6. 2004
    The adenosine diphosphate (ADP) receptor P2Y12 blocking agent clopidogrel is clinically proven to be efficient in preventing thrombotic events...
  62. ncbi Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: a double-blind comparison to clopidogrel with aspirin
    Steen Husted
    Department of Medicine and Cardiology, Arhus University Hospital, Denmark
    Eur Heart J 27:1038-47. 2006
    ..This double-blind, parallel-group study was conducted to assess the pharmacodynamics, pharmacokinetics, and safety of AZD6140, the first oral, reversible adenosine diphosphate (ADP) receptor antagonist...
  63. ncbi Thienopyridines in cardiovascular disease: focus on clopidogrel resistance
    Jolanta Siller-Matula
    3rd Department of Medicine, Cardiology and Emergency Medicine, Wilhelminenhospital, Montleartstrasse 37, A 1160 Vienna, Austria
    Thromb Haemost 97:385-93. 2007
    ..Prasugrel is one of the incoming new drugs with high expectations, but other agents might follow in the near future...
  64. doi P2Y12 receptor-mediated integrin-beta1 activation regulates microglial process extension induced by ATP
    Keiko Ohsawa
    Department of Neurochemistry, National Institute of Neuroscience, Kodaira, Tokyo 187 8502, Japan
    Glia 58:790-801. 2010
    ..These findings indicate that ATP induces the integrin-beta1 activation in microglia through P2Y(12) and suggest that the integrin-beta1 activation is involved in the directional process extension by microglia in brain tissue...
  65. ncbi Perioperative management of patients on adenosine diphosphate inhibitors in the era of drug-eluting stents: review of the literature and clinical implications
    Ali Khoynezhad
    Section for Thoracic and Cardiovascular Surgery, University of Nebraska Medical Center, 982315 Nebraska Medical Center, Omaha, NE 68198 2315, USA
    Curr Med Chem 16:591-8. 2009
    ..They interfere with platelet activation by selectively and irreversibly blocking P2Y12 sub-unit of the adenosine diphosphate receptor on the surface of platelets...
  66. ncbi Initial experience with an intravenous P2Y12 platelet receptor antagonist in patients undergoing percutaneous coronary intervention: results from a 2-part, phase II, multicenter, randomized, placebo- and active-controlled trial
    Adam B Greenbaum
    Henry Ford Heart and Vascular Institute, Detroit, MI, USA
    Am Heart J 151:689.e1-689.e10. 2006
    ..acting, intravenous, specific antagonist of platelet aggregation via binding to the adenosine diphosphate (ADP) P2Y12 receptor subtype...
  67. ncbi Thrombopoietin complements G(i)- but not G(q)-dependent pathways for integrin {alpha}(IIb){beta}(3) activation and platelet aggregation
    Francesca Campus
    Department of Biochemistry, University of Pavia, via Bassi 21, 27100 Pavia
    J Biol Chem 280:24386-95. 2005
    ..aggregation upon blockade of the G(q)-coupled P2Y1 purinergic receptor but not upon inhibition of the G(i)-coupled P2Y12 receptor...
  68. ncbi Molecular modeling of purinergic receptor P2Y12 and interaction with its antagonists
    Chenyang Zhan
    State Key Laboratory of Pharmaceutical Biotechnology, Life College, Nanjing University, Nanjing 210093, China
    J Mol Graph Model 26:20-31. 2007
    ..ADP initiates platelet aggregation by 'simultaneous activation of two G protein-coupled receptors, P2Y1 and P2Y12. P2Y12 has been shown to be the target of the thienopyridine drugs, ticlopidine and clopidogrel...
  69. ncbi [Pharmacogenetics and antiplatelet drugs]
    P Fontana
    Service d angiologie et d hémostase, Departement de Medecine Interne, Faculte de Medecine, Hopital Cantonal Universitaire, 24, Rue Micheli du Crest, 1211 Geneve 14, Suisse
    Rev Med Interne 26:725-32. 2005
    ..The observation of inherited drug response variability gave rise to the field of pharmacogenetics. Pharmacogenetic research on drug targets, particularly platelet enzymes and receptors, is more recent and is becoming an emerging field...
  70. ncbi Aspirin, but not clopidogrel, reduces collateral conductance in a rabbit model of femoral artery occlusion
    Imo E Hoefer
    Research Group for Arteriogenesis, Department of Cardiology, University of Freiburg, Freiburg, Germany
    J Am Coll Cardiol 46:994-1001. 2005
    ..The objective of this study was to test the potential of aspirin and clopidogrel to influence collateral artery growth (arteriogenesis)...
  71. doi Premature preoperative discontinuation of antiplatelet drug therapy in cardiovascular risk patients: a preliminary study on the role of P2Y12 receptor monitoring
    Helfried Metzler
    Department of Anaesthesiology and Intensive Care Medicine, Medical University of Graz, Graz, Austria
    Eur J Anaesthesiol 27:138-45. 2010
    ..New platelet function tests, such as the vasodilator-stimulated phosphoprotein phosphorylation assay, may help to assess the perioperative status of the clopidogrel-specific P2Y12 receptor.
  72. ncbi Pharmacodynamic profile of antiplatelet agents: marked differences between single versus costimulation with platelet activators
    Jochen Graff
    Pharmazentrum Frankfurt, Institute for Clinical Pharmacology, University Hospital Frankfurt am Main, Theodor Stern Kai 7, D 60590 Frankfurt am Main, Germany
    Thromb Res 113:295-302. 2004
    ....
  73. ncbi Scientific and therapeutic insights into the role of the platelet P2Y12 receptor in thrombosis
    Pamela B Conley
    Department of Cardiovascular Biology, Millennium Pharmaceuticals Inc, 256 East Grand Avenue, South San Francisco, CA 94080, USA
    Curr Opin Hematol 10:333-8. 2003
    ..to provide additional clinical benefit to patients with various cardiovascular diseases, especially those who may be aspirin-resistant...
  74. doi Platelet P2Y12 receptor inhibition by thienopyridines: status and future
    Italo Porto
    Catholic University of the Sacred Heart, Cardiovascular Medicine, Largo F Vito, 1, Rome, 00168, Italy
    Expert Opin Investig Drugs 18:1317-32. 2009
    ..Currently, several studies are continuing to test new direct P2Y12 receptor antagonists, such as cangrelor and AZD6140, characterised by a faster reversal of platelet inhibition.
  75. doi Pharmacokinetics and pharmacodynamics of prasugrel, a thienopyridine P2Y12 inhibitor
    Paul P Dobesh
    College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska 68198 6045, USA
    Pharmacotherapy 29:1089-102. 2009
    ..Thus, prasugrel has a pharmacokinetic and pharmacodynamic profile that compares favorably with those of existing antiplatelet agents...
  76. pmc Pharmacokinetic, pharmacodynamic and clinical profile of novel antiplatelet drugs targeting vascular diseases
    Jolanta M Siller-Matula
    Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria
    Br J Pharmacol 159:502-17. 2010
    ..The candidates include various blockers of the purinergic P2Y12 receptor such as prasugrel, an oral irreversible thienopyridine; two adenosine triphosphate analogues that bind ..
  77. ncbi Effect of caffeine on platelet inhibition by clopidogrel in healthy subjects and patients with coronary artery disease
    Eli I Lev
    The Methodist Hospital Research Institute and The Methodist DeBakey Heart Center, Houston, TX 77030, USA
    Am Heart J 154:694.e1-7. 2007
    Clopidogrel inhibits the platelet P2Y12 receptor, leading to increased intracellular cyclic AMP (cAMP) levels. Caffeine also causes a rise in platelet cAMP...
  78. doi Adenosine diphosphate-inducible platelet reactivity shows a pronounced age dependency in the initial phase of antiplatelet therapy with clopidogrel
    T Gremmel
    Division of Angiology, Department of Internal Medicine II, Medical University of Vienna, Vienna, Austria
    J Thromb Haemost 8:37-42. 2010
    ..Like other metabolic processes, the conversion of clopidogrel to its active metabolite may be impaired in older patients, leading to high on-treatment residual ADP-inducible platelet reactivity...
  79. doi Assessment of VerifyNow P2Y12 assay accuracy in evaluating clopidogrel-induced platelet inhibition
    Marie Lordkipanidzé
    Faculties of Pharmacy, Universite de Montreal, Montreal, Canada
    Ther Drug Monit 30:372-8. 2008
    The emergence of point-of-care assays enabling bedside testing such as the VerifyNow P2Y12 system might prove useful in clinical settings...
  80. ncbi Ticagrelor, a platelet aggregation inhibitor for the potential prevention and treatment of arterial thrombosis and acute coronary syndromes
    Sheila A Doggrell
    Queensland University of Technology, School of Life Sciences, GPO Box 2434, Brisbane, QLD4001, Australia
    IDrugs 12:309-17. 2009
    Ticagrelor is an orally active ADP P2Y12 receptor antagonist in development by AstraZeneca plc for the reduction of recurrent ischemic events in patients with acute coronary syndromes (ACS)...
  81. doi Assessment of P2Y(12) inhibition with the point-of-care device VerifyNow P2Y12 in patients treated with prasugrel or clopidogrel coadministered with aspirin
    Christoph Varenhorst
    Uppsala Clinical Research Center, Department Medical Sciences and Cardiology, Uppsala University, Sweden
    Am Heart J 157:562.e1-9. 2009
    ..These tests need to be evaluated in comparison to reference measurements of P2Y(12) function during different thienopyridine treatments...
  82. ncbi Pael receptor, endoplasmic reticulum stress, and Parkinson's disease
    Ryosuke Takahashi
    Laboratory of Motor Neurodegeneration, RIKEN Brain Science Institute BSI, 2 1 Hirosawa, Wako, 351 0198, Saitama, Japan
    J Neurol 250:III25-9. 2003
    ..We found that CHIP enhanced parkinmediated ubiquitination of Pael-R. In concert with Hsp70, CHIP also enhanced the ability of parkin to inhibit cell death induced by Pael-R, indicating that CHIP and Hsp70 are both co-factors of parkin...
  83. ncbi Contribution of protease-activated receptors 1 and 4 and glycoprotein Ib-IX-V in the G(i)-independent activation of platelet Rap1B by thrombin
    Paolo Lova
    Center of Excellence in Applied Biology, Department of Biochemistry, University of Pavia, via Bassi 21, 27100 Pavia
    J Biol Chem 279:25299-306. 2004
    ..A similar effect was also observed upon blockade of the P2Y12 receptor for ADP, as well as in P2Y12 receptor-deficient human platelets, but not after blockade of the P2Y1 ..
  84. ncbi The platelet P2 receptors as molecular targets for old and new antiplatelet drugs
    Christian Gachet
    INSERM U 311, Etablissement Francais du Sang Alsace, 10 rue Spielmann, B P No 36, 67065 Strasbourg Cedex, France
    Pharmacol Ther 108:180-92. 2005
    ..The ATP-gated channel P2X1 and the 2 G protein-coupled P2Y1 and P2Y12 ADP receptors selectively contribute to platelet aggregation...
  85. ncbi Identification of a potent inverse agonist at a constitutively active mutant of human P2Y12 receptor
    Zhongren Ding
    Department of Physiology, Temple University School of Medicine, 3420 N Broad Street, Philadelphia, PA 19140, USA
    Mol Pharmacol 69:338-45. 2006
    ..In conclusion, this is the first report of a cell line stably expressing a constitutively active mutant of human platelet P2Y(12) receptor and the identification of potent inverse agonist...
  86. ncbi The role of ADP receptors in platelet function
    Swaminathan Murugappa
    Department of Physiology, Temple University School of Medicine, Philadelphia, Pennsylvannia 19140, USA
    Front Biosci 11:1977-86. 2006
    ..It is well established that ADP activates platelets through 3 purinergic receptors, namely P2Y1, P2Y12 and P2X1...
  87. ncbi Chemogenomics approaches to G-protein coupled receptor lead finding
    T Klabunde
    Sanofi Aventis Deutschland GmbH, Drug Design, Science and Medical Affairs, Industriepark Hochst, Frankfurt am Main, Germany
    Ernst Schering Res Found Workshop . 2006
    ..of the GPCR collection has provided novel chemical series for several GPCR targets including the adenosine A1, the P2Y12, and the chemokine CCR1 receptor...
  88. doi P2Y12 receptor protein in cortical gray matter lesions in multiple sclerosis
    Susanna Amadio
    Santa Lucia Foundation, Rome, Italy
    Cereb Cortex 20:1263-73. 2010
    ..Our study provides further insights into the pathogenetic features of MS and suggests that the loss of purinergic P2Y(12) receptors might be detrimental to tissue integrity...
  89. ncbi [Update on new antithrombotic treatments]
    F Boehlen
    Unité D Hémostase Service, d angiologie et d hémostase, Département de médicine interne, HUG, Geneve
    Rev Med Suisse 6:109-12. 2010
    ..They are directed either to the P2Y12 receptor or to other original targets...
  90. doi Antagonism of P2Y12 or GPIIb/IIIa receptors reduces platelet-mediated myocardial injury after ischaemia and reperfusion in isolated rat hearts
    José A Barrabés
    Servicio de Cardiologia, Hospital Universitari Vall d Hebron, Passeig Vall d Hebron 119 129, Barcelona, Spain
    Thromb Haemost 104:128-35. 2010
    ..injury after ischaemia and reperfusion in isolated rat hearts and the modification of this effect by the P2Y12 receptor antagonist cangrelor and the glycoprotein IIb/IIIa receptor blocker abciximab...
  91. pmc Ticagrelor: an investigational oral antiplatelet treatment for reduction of major adverse cardiac events in patients with acute coronary syndrome
    Eitan Abergel
    Heart Institute, Rambam Health Care Campus and Technion Israel Institute of Technology, Haifa, Israel
    Vasc Health Risk Manag 6:963-77. 2010
    ..Blockade of the P2Y12 subtype of adenosine diphosphate (ADP) receptor on platelet cell membranes has been established as a key mechanism ..
  92. pmc The P2X1 receptor and platelet function
    Martyn P Mahaut-Smith
    Department of Cell Physiology and Pharmacology, University of Leicester, Leicester, LE1 9HN, UK
    Purinergic Signal 7:341-56. 2011
    ..Platelets express three P2 receptor subtypes, ADP-dependent P2Y1 and P2Y12 G-protein-coupled receptors and the ATP-gated P2X1 non-selective cation channel...
  93. ncbi Comparison of the VASP assay and platelet aggregometry in the evaluation of platelet P2Y12 receptor blockade
    Wiktor Kuliczkowski
    Silesian Center for Heart Diseases, ul Szpitalna 2, Zabrze, Poland
    Pol Arch Med Wewn 121:115-21. 2011
    ..They both showed the predictive value for future adverse events in cardiac patients; however, there are few data that compare these 2 methods...
  94. doi A putative G protein-coupled receptor involved in innate immune defense of Procambarus clarkii against bacterial infection
    Chaohua Dong
    College of Life Science, Qingdao Agricultural University, Qingdao 266109, China
    Comp Biochem Physiol A Mol Integr Physiol 161:95-101. 2012
    ..The results collectively indicated that HP1R was an important immune molecule which was required for red swamp crayfish to defend against bacterial infection...
  95. pmc Real-time imaging reveals that P2Y2 and P2Y12 receptor agonists are not chemoattractants and macrophage chemotaxis to complement C5a is phosphatidylinositol 3-kinase (PI3K)- and p38 mitogen-activated protein kinase (MAPK)-independent
    Katrin Isfort
    Institut fur Physiologie II, Westfalische Wilhelms Universitat Munster, 48149 Munster, Germany
    J Biol Chem 286:44776-87. 2011
    ..We propose that ATP signaling is strictly autocrine or paracrine and that ATP and ADP may act as short-range "touch me" (rather than long-range find me) signals to promote phagocytic clearance via cell spreading...
  96. doi Role of newly formed platelets in thrombus formation in rat after clopidogrel treatment: comparison to the reversible binding P2Y₁₂ antagonist ticagrelor
    Marijke J E Kuijpers
    Dept of Biochemistry, CARIM, Maastricht University, PO Box 616, 6200 MD Maastricht, The Netherlands
    Thromb Haemost 106:1179-88. 2011
    ..This difference is masked by conventional platelet aggregation methods, but is revealed by thrombus formation measurement under flow. Juvenile platelets formed at later time points after clopidogrel treatment promoted thrombus formation...
  97. doi A critical overview on ticagrelor in acute coronary syndromes
    E P Navarese
    Department of Cardiology and Internal Medicine, Ludwik Rydygier Collegium Medicum, Nicolaus Copernicus University, Skłodowskiej Curie Street No 9, 85 094 Bydgoszcz, Poland
    QJM 106:105-15. 2013
    ..therapy in patients with acute coronary syndrome (ACS) was the combination of aspirin and clopidogrel, a P2Y12 receptor inhibitor...
  98. pmc Vascular transcriptional alterations produced by juvenile obesity in Ossabaw swine
    Jaume Padilla
    Biomedical Sciences, University of Missouri, Columbia, Missouri 65211, USA
    Physiol Genomics 45:434-46. 2013
    ..In particular, our results suggest that the oxidized LDL/LOX-1/NF-κB signaling axis may be involved in the early initiation of a juvenile obesity-induced proatherogenic coronary artery phenotype...
  99. doi The ATLAS ACS 2-TIMI 51 trial and the burden of missing data: (Anti-Xa Therapy to Lower Cardiovascular Events in Addition to Standard Therapy in Subjects With Acute Coronary Syndrome ACS 2-Thrombolysis In Myocardial Infarction 51)
    Mori J Krantz
    Division of Cardiology, University of Colorado School of Medicine, Aurora, Colorado, USA
    J Am Coll Cardiol 62:777-81. 2013
    ..in this population, in part because of the expected increased risk in major bleeding by combining aspirin, a P2Y12 receptor inhibitor, and an anticoagulant...
  100. doi Clinical and laboratory significance of defective P2Y(12) pathway function in patients with myeloproliferative neoplasms: a pilot study
    Hung Chang
    Division of Hematology Oncology, Department of Internal Medicine, Chang Gung Memorial Hospital, Taiwan, China
    Acta Haematol 130:181-7. 2013
    ..Two ADP receptors, P2Y1 and P2Y12, are present on platelets...
  101. pmc P2Y4 receptor-mediated pinocytosis contributes to amyloid beta-induced self-uptake by microglia
    Hui Quan Li
    Institute of Neuroscience and Key Laboratory of Neuroscience, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, China
    Mol Cell Biol 33:4282-93. 2013
    ..Recent studies have identified P2Y12 purinergic receptors as triggers for microglial chemotaxis and P2Y6 receptors as mediators for phagocytosis...

Research Grants40

  1. Novel Antithrombotic Diadenosine Tetraphosphate Analogs
    IVAN B YANACHKOV; Fiscal Year: 2010
    ..first time the mechanism of action of this class at the level of the three platelet purinoreceptors (P2X1,P2Y1 and P2Y12), and showed that Ap4A and its analogs antagonize both P2Y1 and P2Y12...
  2. IVAN B YANACHKOV; Fiscal Year: 2015
    ..which inhibit platelet aggregation by a unique new mechanism, targeting both platelet ADP receptors, P2Y1 and P2Y12. Our studies have indicated that this simultaneous targeting might have a synergistic effect on platelet ..
  3. Michael R King; Fiscal Year: 2014
    ..incorporation of additional receptor: ligand interactions required for platelet activation such as GPVI: collagen, P2Y12:ADP, and PAR1:thrombin...
  4. Role of Beta 3 Integrin in Skeletal Metastasis
    Katherine Weilbaecher; Fiscal Year: 2009
    ..unreadable]3 integrin function is modulated by P2Y12, an ADP receptor, and the target of the anti- platelet drug, clopidogrel (Plavix)...
  5. Antiplatelet Therapy: Platelet Inhibition, Polymorphisms, and Protein Biomarkers
    Marc S Sabatine; Fiscal Year: 2012
    ..will be quantified using an assay that specifically assesses an intermediate downstream to activation of the P2Y12 ADP receptor (the target of thienopyridines)...
  6. BLOOD PLATELET THROMBOXANE RECEPTORS
    GUY C LEBRETON; Fiscal Year: 2013
    ..This hypothesis is based on our recent findings that adenosine- based P2Y12 receptor antagonists increase human platelet cAMP levels, and that this increased can account for the bulk of ..
  7. Novel Molecules in Calcium Signaling in Platelets
    Wolfgang Bergmeier; Fiscal Year: 2013
    ..in the absence of CD-GEFI required signaling by protein kinase C (PKC) and the Gai-coupled ADP receptor, P2Y12. The P2Y12 receptor is the target of one of the most successful anti-thrombotic drugs, clopidogrel...
  8. Joshua A Boyce; Fiscal Year: 2016
    ..ADP, an abundant extracellular nucleotide, is the natural ligand for P2Y12 and P2Y1 receptors...
  9. KATHERINE NELSON WEILBAECHER; Fiscal Year: 2014
    ..in platelets and osteoclasts, we will investigate the roles of the [unreadable]3 integrin activating receptor, P2Y12, and a [unreadable]3-integrin stimulating protein, CD47, on platelet and osteoclast function and during bone ..
  10. P2T PURINERGIC RECEPTORS
    JOSE BOYER; Fiscal Year: 2004
    ..of platelet function result from the activation of at least three different receptor subtypes: P2X1, P2Y1 and P2Y AC receptors...
  11. Prolonged and Severe Thrombocytopenia in Neonates
    Pamela Conley; Fiscal Year: 2006
    ..The present application (FastTrack Phase l/ll combination) is designed to develop a novel antagonist of P2Y12 (the ADP receptor on platelets and a validated drug target) that will overcome the limitations of clopidogrel, an ..
  12. P2Y-PURINERGIC RECEPTORS
    T Kendall Harden; Fiscal Year: 2012
    ..An antagonist (clopidogrel;Plavix) of the platelet ADP-activated P2Y12 receptor has made an enormous impact in modern therapeutics, and the potential for drugs that clinically target ..
  13. Role of P2Y Receptors and Activated Platelets in Inflammation
    ANALIA E GARCIA; Fiscal Year: 2012
    ..Clopidogrel (trade name Plavix), antagonizing P2Y12 receptors on platelets, is a widely used potent anti-thrombotic agent...
  14. Joshua A Boyce; Fiscal Year: 2016
    ..We have discovered a molecular pathway through which LTE4 induces pulmonary inflammation (requiring P2Y12 receptors and platelets) and vascular leak (requiring a putative novel LTE4 receptor, GPR99)...
  15. Functional Effects of Adenosine A2A Receptor Activation on Microglia
    STEFKA IVANOVA GYONEVA; Fiscal Year: 2012
    ..This directional process extension is mediated by ATP released from damaged cells and activation of P2Y12 receptors on microglia...
  16. Thrombin signaling in Hemostatis and thrombosis
    Shaun R Coughlin; Fiscal Year: 2010
    ..Genetic and pharmacological approaches will be used. PAR interactions with P2Y12 and Tbxa2r (TP) will also be probed...
  17. Novel Mechanisms of Visceral Pain: Functional Properties of Microglia
    Jennifer L Watts; Fiscal Year: 2012
    ..state characterized by increased expression of CDIIb and Ibal proteins and membrane purinergic receptors (P2X4 and P2Y12) and 2) To show that colon-inflammation induced visceral hypersensitivity is reversed by inhibiting microglia with ..
  18. Thomas H Smith; Fiscal Year: 2015
    ..There is limited evidence in the literature that suggests PAR4 forms heterodimers with P2Y12. I will address this question using biochemical approaches and sophisticated imaging techniques in order provide ..
  19. FEDIAS LEONTIOU CHRISTOFI; Fiscal Year: 2015
    ..Negative autocrine signals are transduced through P2Y12 and A3R. 'Plurichemical'purinergic transmission occurs in the human ENS...
  20. James Palis; Fiscal Year: 2016
    ..These functional studies correlate with the differential upregulation of PAR1 and down-regulation of P2Y12 in primary embryonic versus adult platelets...
  21. Cysteinyl leukotriene signaling in proliferation, cytokine production and PGD2 ge
    Sailaja Paruchuri; Fiscal Year: 2010
    ..Blocking PPAR3 or P2Y12 receptor abrogates LTE4-induced MIP-12 generation as well as PGD2 response in LAD2 cells...
  22. Pro- and Anti-Nociceptive Actions of P2y Nucleotide Receptors in Sensory Neurons
    Derek C Molliver; Fiscal Year: 2010
    ..Specific Aim 3 will examine the contribution of P2Y ADP receptors to behavioral pain response thresholds in vivo and will determine whether pharmacological or genetic ..
  23. Purinergic Regulation of the Renal Microcirculation
    Edward W Inscho; Fiscal Year: 2012
    ..Ang II hypertension, and P2Y12 receptor activation, contribute to inflammation and fibrosis and converge on a loss of autoregulatory efficiency...
  24. Cys-LT signaling in proliferation, cytokine production and PGD2 generation of MCs
    Sailaja Paruchuri; Fiscal Year: 2012
    ..Blocking PPAR[unreadable] or P2Y12 receptor abrogates LTE4-induced MIP-1[unreadable] generation as well as PGD2 response in LAD2 cells...
  25. Functional G Protein pathways in platelet activation
    Satya P Kunapuli; Fiscal Year: 2010
    ..These studies will enhance our understanding of the signaling pathways and their role in platelet activation, and might identify potential newer targets for the treatment of thrombosis. ..
  26. Platelet ADP receptors
    Satya Kunapuli; Fiscal Year: 2008
    ..During the previous grant period, we have demonstrated 3 ADP receptor subtypes, P2Y1, P2Y12, and P2X1, on platelets and elucidated a number of signaling mechanisms in platelets...
  27. NUCLEOTIDE-MEDIATED LEUKOCYTE STIMULATION
    Satya Kunapuli; Fiscal Year: 2004
    ..The studies proposed in this application will also help us understand the mechanisms of neutrophil activation and contribute to the knowledge of better treatments and to the design of therapeutics for inflammatory diseases. ..
  28. Arachidonic Acid Metabolism in Blood and Vascular Cells
    Jun Yang Liou; Fiscal Year: 2006
    ..Information provided by studies from this renewal application will have great impact on understanding the fundamental cytoprotection process and offer an excellent opportunity for developing new therapeutic agents. ..
  29. EICOSANOIDS AND NO IN CEREBROVASCULAR THROMBOSIS
    Kenneth Wu; Fiscal Year: 2003
    ..It is intended that this program will enable several laboratories to work individually and together to achieve the highest degree of innovating and productivity. ..
  30. Fish as Genetic Models for Aging
    Pudur Jagadeeswaran; Fiscal Year: 2002
    ..These results will also serve as preliminary data for a future NIH R01 grant application focusing on screening of Cynolebias mutants for long life span. ..
  31. SATURATION MUTAGENESIS OF ZEBRAFISH COAGULATION PATHWAY
    Pudur Jagadeeswaran; Fiscal Year: 2003
    ..Identification of human homologues will further our understanding of how the coagulation cascade functions in vivo, suggest novel targets for antithrombotic therapy and provide candidate genetic markers for thrombotic disease. ..
  32. MOLECULAR BIOLOGY OF COLLAGEN RECEPTORS
    Thomas Kunicki; Fiscal Year: 2004
    ..The successful completion of the proposed studies will lead to a substantial increase in our understanding of the genetics and physiology of the platelet collagen receptor, GPVI. ..
  33. Novel Antithrombotic Diadenosine Tetraphosphate Analogs
    Ivan Yanachkov; Fiscal Year: 2007
    ..Existing data suggest P2Y1 targeting, but do not rule out P2Y12 inhibition as well...
  34. Trafficking/signaling of P2Y receptors in polarized epithelial cells
    Robert A Nicholas; Fiscal Year: 2011
    ..Our studies will provide novel and important information on the cellular mechanisms of P2Y receptor targeting and the regulation of P2Y receptor signaling activity in epithelial cells. ..
  35. Diadenosine Boranotetraphosph(on)ates as Antithrombotic Drugs
    Ivan Yanachkov; Fiscal Year: 2007
    ..Existing data suggest P2Y1 targeting, but does not rule out P2Y12 inhibition as well...
  36. Molecular Genetics of Integrin Collagen Receptors
    Thomas Kunicki; Fiscal Year: 2007
    ..From a clinical standpoint, these studies will also reveal the impact of these gene differences on risk for adverse events in bleeding disorders such as Von Willebrand Disease. ..
  37. Mechanisms of antibiotic action in Neisseria gonorrhoeae.
    Robert A Nicholas; Fiscal Year: 2010
    ..Together, these projects utilize genetic, biochemical, biophysical, and proteomics approaches to generate new insights into the mechanisms of antibiotic action in N. gonorrhoeae. ..
  38. Role of Young Thrombocytes and Their Microparticles
    Pudur Jagadeeswaran; Fiscal Year: 2008
    ..Such studies should provide insight into the role of platelet microparticles in hemostasis, mechanisms of their production and platelet maturation. ..