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Purification and Functional Reconstitution of the Human P2Y12 Receptor
Molecular Pharmacology, 2003The human P2Y12 receptor (P2Y12-R) is a member of the G protein coupled P2Y receptor family, which is intimately involved in platelet physiology. We describe here the purification and functional characterization of recombinant P2Y12-R after high-level expression from a baculovirus in Sf9 insect cells.
Erik T, Bodor +5 more
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Switching Platelet P2Y12 Receptor Inhibiting Therapies
Interventional Cardiology ClinicsAntiplatelet therapy involving aspirin and a P2Y12 receptor inhibitor is fundamental in managing patients with atherothrombotic disease. Switching between P2Y12 inhibitors is frequently observed in clinical settings for various reasons, such as safety, efficacy, patient adherence, or cost concerns.
Luis, Ortega-Paz +4 more
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Pharmacokinetics and Pharmacodynamics of Approved and Investigational P2Y12 Receptor Antagonists
Clinical Pharmacokinetics, 2020Coronary artery disease remains the major cause of mortality worldwide. Antiplatelet drugs such as acetylsalicylic acid and P2Y12 receptor antagonists are cornerstone treatments for the prevention of thrombotic events in patients with coronary artery disease.
Uta Schilling +2 more
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AbstractThrombosis, or the formation of blood clots, can lead to serious medical conditions such as stroke, heart attack, and deep vein thrombosis. The purinoreceptor P2Y12 plays a critical role in the thrombotic pathway and is targeted for therapy to prevent clot formation.
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Efficacy and Safety of Ticagrelor: A Reversible P2Y12 Receptor Antagonist
Annals of Pharmacotherapy, 2010Objective: To summarize the pharmacokinetic and pharmacodynamic properties of ticagrelor, a selective P2Y12 receptor antagonist, and evaluate its role in the treatment of patients with acute coronary syndromes (ACS).
Shawn D, Anderson +3 more
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Decreased platelet inhibition by P2Y12 receptor blockers in anaemia
European Journal of Clinical Investigation, 2017AbstractBackgroundAnaemic patients undergoing angioplasty and stenting are at an increased risk of ischaemic events, which may be caused by an inadequate response to antiplatelet therapy with adenosine diphosphate (ADP) P2Y12 inhibitors. In the current study, we investigated the associations between anaemia and on‐treatment platelet reactivity in ...
Patricia P. Wadowski +8 more
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The P2Y12 receptor: no active metabolite, no party
Nature Reviews Cardiology, 2009Poor responders to clopidogrel have low levels of circulating active metabolite. However, in vitro experiments have shown that blood platelets from poor responders are fully inhibited by the active metabolite of this prodrug. Impaired platelet inhibition reflects inadequate plasma levels of active metabolites, and not differences in platelet P2Y12 ...
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The role of P2Y12 receptor in ischemic stroke of atherosclerotic origin
Cellular and Molecular Life Sciences, 2018Atherosclerosis is a chronic and progressive disease of the arterial walls and a leading cause of non-cardioembolic ischemic stroke. P2Y12 is a well-recognized receptor that is expressed on platelets and is a target of thienopyridine-type antiplatelet drugs.
Ying, Gao +4 more
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Structure, Pharmacology and Roles in Physiology of the P2Y12 Receptor
2017P2Y receptors are G-protein-coupled receptors (GPCRs) for extracellular nucleotides. The platelet ADP-receptor which has been denominated P2Y12 receptor is an important target in pharmacotherapy. The receptor couples to Gαi2 mediating an inhibition of cyclic AMP accumulation and additional downstream events including the activation of ...
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Platelet P2Y12 Receptor Inhibition
American Journal Cardiovascular Drugs, 2010David Vivas, Dominick J. Angiolillo
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