PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 11454254-3 2001 The thienopyridines, ticlopidine and clopidogrel, act, via metabolites, on the platelet ADP receptor subtype now designated P2Y(12 )(formerly P(2T), P2T (AC), P2Y (ADP) or P2Y(cyc)) and these agents have proven clinical efficacy. Thienopyridines 4-19 purinergic receptor P2Y12 Homo sapiens 159-168 14717977-1 2004 The P2Y12 ADP receptor is one of the major regulators of platelet activation and the target of antithrombotic thienopyridines (ticlopidine and clopidogrel). Thienopyridines 110-125 purinergic receptor P2Y12 Homo sapiens 4-9 14684289-1 2004 Novel classes of thienopyrimidines and thienopyridines have been identified as potent inhibitors of VEGFR-2 kinase. Thienopyridines 39-54 kinase insert domain receptor Homo sapiens 100-107 14610915-4 2003 P2Y12 inhibits adenylyl cyclase through a glycoprotein i (Gi)-dependent pathway, and is the target of the clinically used thienopyridines, ticlopidine (Ticlid, F. Hoffman-La Roche) and clopidogrel (Plavix, Bristol-Myers Squibb/Sanofi-Synthelabo). Thienopyridines 122-137 purinergic receptor P2Y12 Homo sapiens 0-5 11454254-3 2001 The thienopyridines, ticlopidine and clopidogrel, act, via metabolites, on the platelet ADP receptor subtype now designated P2Y(12 )(formerly P(2T), P2T (AC), P2Y (ADP) or P2Y(cyc)) and these agents have proven clinical efficacy. Thienopyridines 4-19 purinergic receptor P2Y12 Homo sapiens 172-180 31590445-7 2019 We used this assay to characterize a series of thienopyridines with in vitro bone anabolic activity, one of which was identified as a selective CDK8/19 inhibitor. Thienopyridines 47-62 cyclin dependent kinase 8 Homo sapiens 144-151 11192941-1 2000 We propose that anti-platelet thienopyridines, such as ticlopidine or clopidogrel, are thrombolytic owing to endothelial release of prostacyclin (PGI2) and tissue plasminogen activator (t-PA). Thienopyridines 30-45 plasminogen activator, tissue type Rattus norvegicus 156-190 34731765-3 2022 Despite that P2Y12 platelets" receptor is an excellent target for developing antiplatelet agents, only five approved medications are currently in clinical use which are classified into thienopyridines and nucleoside-nucleotide derivatives. Thienopyridines 185-200 purinergic receptor P2Y12 Homo sapiens 13-18 33335655-0 2020 Novel Thienopyridines as RIPK2 Inhibitors for Treating Inflammatory Bowel Disease. Thienopyridines 6-21 receptor interacting serine/threonine kinase 2 Homo sapiens 25-30 31590445-8 2019 Thienopyridines inhibited luciferase induction in the WT but not dKO cells and their IC50 values in the WT reporter assay showed near-perfect correlation (R2 = 0.98) with their reported activities in a bone anabolic activity assay, confirming that the latter function is mediated by CDK8/19 and validating our assay as a robust and quantitative method for CDK8/19 inhibition. Thienopyridines 0-15 cyclin dependent kinase 8 Homo sapiens 356-363 31590445-8 2019 Thienopyridines inhibited luciferase induction in the WT but not dKO cells and their IC50 values in the WT reporter assay showed near-perfect correlation (R2 = 0.98) with their reported activities in a bone anabolic activity assay, confirming that the latter function is mediated by CDK8/19 and validating our assay as a robust and quantitative method for CDK8/19 inhibition. Thienopyridines 0-15 cyclin dependent kinase 8 Homo sapiens 283-290 27548273-8 2017 Patients discharged with ticagrelor versus thienopyridines demonstrated a higher rate of crossover to other P2Y12 inhibitors (11 vs. 5%, p = 0.03). Thienopyridines 43-58 purinergic receptor P2Y12 Homo sapiens 108-113 29710801-1 2018 The thienopyridines class of drugs used as P2Y12 receptor antagonists plays a vital role in antiplatelet therapy. Thienopyridines 4-19 purinergic receptor P2Y12 Rattus norvegicus 43-48 25443875-3 2014 We hypothesised that thienopyridines expose the free thiol group once acidified (by the stomach) before biotransformation into active metabolites, and in the presence of nitrite (from saliva and the stomach) to form nitrosothiol derivatives (Thienopyridine induced-SNO formation). Thienopyridines 21-36 strawberry notch homolog 1 Homo sapiens 265-268 26758983-3 2016 P2Y12 receptor antagonists, thienopyridines and ticagrelor, differ in their mode of action being prodrugs instead of direct acting and irreversibly instead of reversibly binding to P2Y12 . Thienopyridines 28-43 purinergic receptor P2Y12 Homo sapiens 0-5 26758983-3 2016 P2Y12 receptor antagonists, thienopyridines and ticagrelor, differ in their mode of action being prodrugs instead of direct acting and irreversibly instead of reversibly binding to P2Y12 . Thienopyridines 28-43 purinergic receptor P2Y12 Homo sapiens 181-186 26270719-2 2016 As cangrelor is administered intravenously, it is necessary to switch to an oral P2Y12 antagonist following PCI, such as the thienopyridines clopidogrel, and prasugrel or the non-pyridine ticagrelor. Thienopyridines 125-140 purinergic receptor P2Y12 Homo sapiens 81-86 26444255-5 2016 Cangrelor blocks the binding to the platelet P2Y12 receptor of the active metabolite of the thienopyridines, clopidogrel and prasugrel. Thienopyridines 92-107 purinergic receptor P2Y12 Homo sapiens 45-50 25443875-4 2014 We have performed in vitro studies with each of the thienopyridines tablets/compounds confirming direct Th-SNO formation from the parent (inactive) drug by the following mechanism. Thienopyridines 52-67 strawberry notch homolog 1 Homo sapiens 107-110 24142066-1 2014 Thienopyridines are a class of antiplatelet drugs that are metabolized in the liver to several metabolites, of which only one active metabolite can irreversibly antagonize the platelet P2Y12 receptor. Thienopyridines 0-15 purinergic receptor P2Y, G-protein coupled 12 Mus musculus 185-190 24845219-3 2014 Considering the importance of P2Y12 receptor in platelet function, a class of antiplatelet drugs, thienopyridines, have been designed and successfully used to prevent thrombosis. Thienopyridines 98-113 purinergic receptor P2Y12 Homo sapiens 30-35 24845219-8 2014 P2Y12 receptor may also be expressed in other cells of the immune system, indicating that thienopyridines could directly influence the immune system rather than only through platelets. Thienopyridines 90-105 purinergic receptor P2Y12 Homo sapiens 0-5 23476040-0 2013 Impaired platelet P2Y12 inhibition by thienopyridines in chronic kidney disease: mechanisms, clinical relevance and pharmacological options. Thienopyridines 38-53 purinergic receptor P2Y12 Homo sapiens 18-23 23925438-8 2013 In conclusion, ELISA-VASP is a fast, easy-to-use and specific test to identify HPR in ACS patients on thienopyridines. Thienopyridines 102-117 vasodilator stimulated phosphoprotein Homo sapiens 21-25 25163670-4 2014 Thienopyridines are class of drugs that specifically and irreversibly inhibit the P2Y12 receptor. Thienopyridines 0-15 purinergic receptor P2Y12 Homo sapiens 82-87 22963529-2 2013 The first family of adenosine diphosphate P2Y12 receptors inhibiting drug is represented by thienopyridines and among these ticlopidine was the first approved by Food and Drug Administration; actually its use is discouraged because of its potential side effects (neutropenia, anemia, gastrointestinal distress and thrombotic thrombocytopenic purpura). Thienopyridines 92-107 purinergic receptor P2Y12 Homo sapiens 42-47 23816027-2 2013 BACKGROUND: It has been suggested that LTA and VASP-P assay correlate differently according to the level of P2Y12 receptor blockade by thienopyridines. Thienopyridines 135-150 vasodilator stimulated phosphoprotein Homo sapiens 47-51 23816027-2 2013 BACKGROUND: It has been suggested that LTA and VASP-P assay correlate differently according to the level of P2Y12 receptor blockade by thienopyridines. Thienopyridines 135-150 purinergic receptor P2Y12 Homo sapiens 108-113 21946108-1 2011 Thienopyridines (ticlopidine, clopidogrel and prasugrel) are pro-drugs that require metabolism to exhibit a critical thiol group in the active form that binds to the P2Y12 receptor to inhibit platelet activation and prevent thrombus formation in vivo. Thienopyridines 0-15 purinergic receptor P2Y12 Homo sapiens 166-171 23617077-0 2013 A QSAR and molecular modeling study on a series of 3, 4-dihydro-1-isoquinolinamines and thienopyridines acting as nitric oxide synthase inhibitors. Thienopyridines 88-103 nitric oxide synthase 1 Homo sapiens 114-135 22974536-1 2012 BACKGROUND: A recent clinical trial has demonstrated that patients with acute coronary syndromes (ACS) and the reduced function allele CYP2C19*2 (*2 allele), who are treated with thienopyridines, have an increased risk of adverse cardiac events with clopidogrel, but not with prasugrel. Thienopyridines 179-194 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 135-142 22918731-2 2012 Among the P2Y12 receptor inhibitors, the group of thienopyridines include ticlopidine, clopidogrel and prasugrel, all of which are orally administered prodrugs leading to irreversible P2Y12 receptor inhibition. Thienopyridines 50-65 purinergic receptor P2Y12 Homo sapiens 10-15 22918731-2 2012 Among the P2Y12 receptor inhibitors, the group of thienopyridines include ticlopidine, clopidogrel and prasugrel, all of which are orally administered prodrugs leading to irreversible P2Y12 receptor inhibition. Thienopyridines 50-65 purinergic receptor P2Y12 Homo sapiens 184-189 21822146-7 2011 Clopidogrel-chloride-SNO displayed rapid-release kinetics in a chemical environment, which was reflected by immediate and transient vasorelaxation when compared with the SNO derivatives of the other thienopyridines. Thienopyridines 199-214 strawberry notch homolog 1 Homo sapiens 21-24 21822146-10 2011 Differences in SNO yield and vasoactivity exist between thienopyridine preparations that might be important to our understanding of the direct pharmacological effectiveness of thienopyridines on vascular and platelet function. Thienopyridines 176-191 strawberry notch homolog 1 Homo sapiens 15-18 21828263-6 2011 These studies show that, in vitro, CYP3A4/5, 2C19, and 2B6 are individually capable of converting clopidogrel and prasugrel to the AM and that the cytochrome P450 preference for these two thienopyridines is very similar. Thienopyridines 188-203 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-49 21826477-2 2011 The available thienopyridines are prodrugs and must be converted into active forms by the cytochrome P450 (CYP) enzyme system. Thienopyridines 14-29 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 90-105 21826477-2 2011 The available thienopyridines are prodrugs and must be converted into active forms by the cytochrome P450 (CYP) enzyme system. Thienopyridines 14-29 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 107-110 21074424-0 2010 Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors. Thienopyridines 29-44 checkpoint kinase 1 Homo sapiens 55-59 21447613-7 2011 In conclusion, the TI of thienopyridines in the mouse may be decreased by P2Y(12)-independent off-target effects at the vessel wall, whereas that of elinogrel may be enhanced by the reversible, competitive nature of the antiplatelet agent. Thienopyridines 25-40 purinergic receptor P2Y, G-protein coupled 12 Mus musculus 74-81 20210760-3 2010 As a result, this receptor has been a target for the development of clinically effective antiplatelet agents, such as the thienopyridines ticlopidine and, more recently, clopidogrel, the only two currently FDA-approved P2Y12 antagonists. Thienopyridines 122-137 purinergic receptor P2Y12 Homo sapiens 219-224 21073556-3 2010 Other interactions between thienopyridines and CYP3A4/5 have also been reported for statins and calcium channel blockers. Thienopyridines 27-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53 20977287-5 2010 On the other hand, thienopyridines suppress the platelet aggregation adenosine diphosphate (ADP) pathway by inhibiting the platelet P2Y12 subtype of the ADP receptor. Thienopyridines 19-34 purinergic receptor P2Y12 Homo sapiens 132-137 19946242-3 2009 Thienopyridines are a class of drugs that function via inhibition of the adenosine diphosphate (ADP) P2Y12 platelet receptors. Thienopyridines 0-15 purinergic receptor P2Y12 Homo sapiens 101-106 22282698-5 2010 Recent investigations have included ticagrelor, a reversible inhibitor of the P2Y12 platelet receptor, which appears to have overcome several drawbacks of the current thienopyridines. Thienopyridines 167-182 purinergic receptor P2Y12 Homo sapiens 78-83 19882081-0 2009 P2Y12 inhibitors: thienopyridines and direct oral inhibitors. Thienopyridines 18-33 purinergic receptor P2Y12 Homo sapiens 0-5 17635731-3 2007 In contrast to aspirin, studies that used specific tests to measure the pharmacological effect of thienopyridines [e.g. vasodilator-stimulated phosphoprotein (VASP)] showed a wide variability of responses to these drugs, with significant proportions of subjects (15-30%) who are very poor responders. Thienopyridines 98-113 vasodilator stimulated phosphoprotein Homo sapiens 120-157 19678800-0 2009 Platelet P2Y12 receptor inhibition by thienopyridines: status and future. Thienopyridines 38-53 purinergic receptor P2Y12 Homo sapiens 9-14 17635731-3 2007 In contrast to aspirin, studies that used specific tests to measure the pharmacological effect of thienopyridines [e.g. vasodilator-stimulated phosphoprotein (VASP)] showed a wide variability of responses to these drugs, with significant proportions of subjects (15-30%) who are very poor responders. Thienopyridines 98-113 vasodilator stimulated phosphoprotein Homo sapiens 159-163 17234410-0 2007 Discovery of thienopyridines as Src-family selective Lck inhibitors. Thienopyridines 13-28 LCK proto-oncogene, Src family tyrosine kinase Homo sapiens 53-56 17234410-0 2007 Discovery of thienopyridines as Src-family selective Lck inhibitors. Thienopyridines 13-28 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 32-35 17580012-3 2007 STUDY SELECTION: We included randomized controlled trials that assessed the clinical efficacy (risk of death or infarction) and safety (bleeding and thrombocytopenia) of GPIIb/IIIa inhibitors in patients pretreated with thienopyridines. Thienopyridines 220-235 integrin subunit alpha 2b Homo sapiens 170-175 17580012-7 2007 CONCLUSIONS: Use of GPIIb/IIIa inhibitors reduces the risk of adverse cardiac events in NSTEACS patients pre-treated with aspirin and thienopyridines but increases the risk of severe bleeding and thrombocytopenia. Thienopyridines 134-149 integrin subunit alpha 2b Homo sapiens 20-25 17234410-2 2007 These thienopyridines were designed based on a desire to access the unique residues in the extended hinge region of Lck. Thienopyridines 6-21 LCK proto-oncogene, Src family tyrosine kinase Homo sapiens 116-119 16194206-6 2005 Conversely, secreted ADP strongly potentiated Rac activation induced by FcgammaRIIa clustering or TRAP via its P2Y12 receptor, the target of antithrombotic thienopyridines. Thienopyridines 156-171 AKT serine/threonine kinase 1 Homo sapiens 46-49 17187456-8 2007 Two direct and reversible P2Y12 antagonists, cangrelor and AZD6140, have very rapid onset and reversal of platelet inhibition, which make them attractive alternatives to thienopyridines, especially when rapid inhibition of platelet aggregation or its quick reversal are required. Thienopyridines 170-185 purinergic receptor P2Y12 Homo sapiens 26-31 16941047-8 2006 Two direct and reversible P2Y(12) antagonists, cangrelor and AZD6140, feature very rapid onset and reversal of platelet inhibition, which make them attractive alternatives to thienopyridines, especially when rapid inhibition of platelet aggregation or its quick reversal are required. Thienopyridines 175-190 purinergic receptor P2Y12 Homo sapiens 26-33 17066149-8 2006 Two direct and reversible P2Y12 antagonists, cangrelor and AZD6140, feature very rapid onset and reversal of platelet inhibition, which make them attractive alternatives to thienopyridines, especially when rapid inhibition of platelet aggregation or its quick reversal are required. Thienopyridines 173-188 purinergic receptor P2Y12 Homo sapiens 26-31 16194206-6 2005 Conversely, secreted ADP strongly potentiated Rac activation induced by FcgammaRIIa clustering or TRAP via its P2Y12 receptor, the target of antithrombotic thienopyridines. Thienopyridines 156-171 purinergic receptor P2Y12 Homo sapiens 111-116 15816504-4 2005 The thienopyridines (ticlopidine, clopidogrel and prasugrel) irreversibly inactivate the P2Y12 receptor via the covalent binding of an active metabolite generated in the liver, while the other compounds are competitive antagonists. Thienopyridines 4-19 purinergic receptor P2Y, G-protein coupled 12 Mus musculus 89-94 16353041-16 2005 CONCLUSION: In pts with NSTEACS both thienopyridines attenuated acute phase elevation of vWF. Thienopyridines 37-52 von Willebrand factor Homo sapiens 89-92