ライフサイエンスコーパス: P2Y(12) receptor

1 in was potentiated by ADP acting through the P2Y12 receptor.

2 largely independent of signaling through the P2Y12 receptor.

3 lepsy or peritumoral cortex tissue expressed P2Y12 receptors.

4 y active, and its activity is potentiated by P2Y12 receptors.

5 ATP release, and microglial response through P2Y12 receptors.

6 d an autocrine ADP-mediated response through P2Y12 receptors.

7 addition to that derived from antagonism of P2Y12 receptors.

8 CysLT1R and CysLT2R but not in mice lacking P2Y12 receptors.

9 onal activation and blocked by inhibition of P2Y12 receptors.

10 ing that they do not directly antagonize the P2Y(12) receptor.

11 of the functional responses of the platelet P2Y(12) receptor.

12 ically among these mutants and the wild-type P2Y(12) receptor.

13 h the extracellular cysteine residues on the P2Y(12) receptor.

14 ated by adenosine-5'-diphosphate through the P2Y(12) receptor.

15 receptor present on platelets, that is, the P2Y(12) receptor.

16 ) to ADP, the specific agonist of P2Y(1) and P2Y(12) receptors.

17 ressing high levels of recombinant P2Y(2) or P2Y(12) receptors.

18 naling pathways linked to the P2X4, P2X7 and P2Y(12) receptors.

19 The P2Y(12) receptor, activated by ADP, plays a central role

20 ependent in part on G(i) stimulation through P2Y(12) receptor activation by secreted ADP.

21 d in the initiation of platelet aggregation, P2Y12 receptor activation appears to account for the bul

22 process outgrowth to damaged tissue requires P2Y12 receptor activation but is unaffected by blocking

23 Furthermore, we show that P2Y12 receptor activation is not required for protease-a

24 osine 5'-triphosphate), an antagonist of the P2Y(12) receptor, also did not differ dramatically among

25 rugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the

26 The cloning of the P2Y(12) receptor and its subsequent knockout in mice pro

27 nstitutively active mutant of human platelet P2Y(12) receptor and the identification of potent invers

28 X-ray crystal structures for the P2Y(1) and P2Y(12) receptors and homology modeling has stimulated r

29 of a local thrombus, dual inhibition of the P2Y12 receptor and calcium mobilization result in a comp

30 ivation markers including CD45, CD11b/c, and p2y12 receptor and evaluated their activation state usin

31 is dependent on both the G(alpha)(i)-coupled P2Y12 receptor and the G(alpha)(q)-coupled P2Y1 receptor

32 mole inhibit platelet function by inhibiting P2Y12 receptors and platelet phosphodiesterase, respecti

33 de bridges with both Cys17 and Cys270 in the P2Y(12) receptor, and thereby inactivate the receptor.

34 y symptoms during aspirin-induced reactions, P2Y(12) receptor antagonism with prasugrel completely in

35 lular traps had little effects, but platelet P2Y12 receptor antagonism with clopidogrel, fibrinolysis

36 supporting pleiotropic effects coupled with P2Y12 receptor antagonism.

37 A protein kinase C inhibitor GF 109203X or a P2Y(12) receptor antagonist AR-C69931MX partly reduced G

38 AZD6140 is a reversible oral P2Y(12) receptor antagonist that has been studied in ACS

39 Ticagrelor is a P2Y(12) receptor antagonist that showed superior clinica

40 s a potent, highly selective, and reversible P2Y(12) receptor antagonist with a rapid onset and short

41 47, LY640315), a novel potent thienopyridine P2Y(12) receptor antagonist, has the potential to achiev

42 agrelor is the first reversibly binding oral P2Y(12) receptor antagonist.

43 s a potent, highly selective, and reversible P2Y12 receptor antagonist and by far the most potent inh

44 ubstituents on the ribose and base conferred P2Y12 receptor antagonist properties to these molecules

45 The direct-acting platelet P2Y12 receptor antagonist ticagrelor can reduce the inci

46 The P2Y12 receptor antagonist ticagrelor has been shown to b

47 escribed an additional mode of action of the P2Y12 receptor antagonist ticagrelor.

48 On the other hand, apyrase, the P2Y12 receptor antagonist, AR-C67085, and indomethacin o

49 However, pretreatment of platelets with P2Y12 receptor antagonist, AR-C69331MX did not interfere

50 on of platelets with aspirin, but not with a P2Y12 receptor antagonist, caused a marked reduction in

51 d by either the integrin inhibitor RGDS or a P2Y12 receptor antagonist, indicating a requirement for

52 Physicians considering prescription of P2Y12-receptor antagonist for long-term (>1 year) protec

53 heral arterial disease, or following a brief P2Y12-receptor antagonist interruption, whereas clopidog

54 platelet inhibitory effects induced by oral P2Y(12) receptor antagonists are delayed in patients wit

55 Oral P2Y(12) receptor antagonists exhibit delayed onset of pl

56 in platelet activation and is the target of P2Y(12) receptor antagonists that have proven therapeuti

57 Platelet inhibitory effects induced by oral P2Y12 receptor antagonists are delayed in patients with

58 lar patients who smoke benefit from platelet P2Y12 receptor antagonists more than their nonsmoking pe

59 ntagonists), cyclopentyltriazolopyrimidines (P2Y12 receptor antagonists), anti-von Willebrand factor

60 al study, consisting of the thienopyridines (P2Y12 receptor antagonists), cyclopentyltriazolopyrimidi

61 morphine and its potential interactions with P2Y12 receptor antagonists, as well as on the central is

62 P2Y12 receptor antagonists, concurrently administered wi

63 It was suppressed by P2Y12 receptor antagonists, which also reduced process l

64 lial process extension, which was blocked by P2Y12 receptor antagonists.

65 As head-to-head comparative trials between P2Y12-receptor antagonists are lacking, selection of a s

66 r and inside-out signaling from the P2Y1 and P2Y12 receptors are necessary for phospholipase A(2) act

67 Platelet P2Y12 receptors are the targets of very widely used anti

68 namides, which are potent antagonists of the P2Y12 receptor, are presented.

69 Prasugrel P2Y(12) receptor blockade is associated with greater pha

70 Upstream Strategy for the Administration of P2Y(12) Receptor Blockers In Non-ST Elevated Acute Coron

71 The powerful antithrombotic effects of P2Y12 receptor blockers may, in part, be mediated by pro

72 P did not require Gi signaling or functional P2Y12 receptors but was mediated through activation of a

73 the reactive cysteine residues on the human P2Y(12) receptor by site-directed mutagenesis using pCMB

74 Both P2Y1 and P2Y12 receptors can also undergo PMA-stimulated internal

75 eas pharmacological blockade of G(i)-coupled P2Y12 receptors decreased sleep.

76 In platelets from a P2Y12 receptor-defective patient, alpha-thrombin, SFLLRN

77 duced changes at somatic junctions triggered P2Y12 receptor-dependent microglial neuroprotection, reg

78 rful synergism is explained by blockade of a P2Y12 receptor-dependent, NO/cGMP-insensitive phosphatid

79 Cys97Ser and Cys175Ser mutants of the P2Y(12) receptor did not express when transfected into C

80 epinephrine (alpha(2A)-adrenergic) and ADP (P2Y12) receptors display strong preferences among G(i) f

81 thus reduces surveillance, whereas blocking P2Y12 receptors does not affect membrane potential, rami

82 Here we show that blockade of platelet P2Y12 receptors dramatically enhances the antiplatelet p

83 hat microglia from mice lacking G(i)-coupled P2Y(12) receptors exhibit normal baseline motility but a

84 P2Y12 receptor expression by LAD2 cells is required for

85 P2Y12 receptor expression permits LTE4-induced activatio

86 26 directly and indirectly affects ADAM9 and P2Y12 receptor expression.

87 idges linking its extracellular domains, the P2Y(12) receptor has 2 free cysteines in its extracellul

88 As the P2Y(12) receptor has been shown to activate G protein-ga

89 number of small-molecule antagonists for the P2Y(12) receptor have received approval for their clinic

90 pCMBS inactivated the wild-type P2Y(12) receptor in a concentration-dependent manner, wh

91 ls are important functional effectors of the P2Y(12) receptor in human platelets.

92 The discovery of the role of P2Y(12) receptor in platelet aggregation leads to a new

93 The role of the G(i)-coupled platelet P2Y(12) receptor in platelet function has been well esta

94 Activation by ADP of both P2Y(1) and P2Y(12) receptors in platelets contributes to platelet a

95 ently identified functional effector for the P2Y12 receptor, in the regulation of ADP-induced TXA2 ge

96 ls of inhibition of platelet aggregation via P2Y(12) receptor inhibition, not only for the prevention

97 treatment platelet reactivity and incomplete P2Y12 receptor inhibition are risk factors for SAT.

98 stenting and treatment strategies to improve P2Y12 receptor inhibition in patients with high post-tre

99 phoprotein phosphorylation levels to measure P2Y12 receptor inhibition were determined (n = 20) and c

100 pidogrel metabolism, potentially attenuating P2Y12 receptor inhibition.

101 ual antiplatelet therapy with aspirin plus a P2Y(12) receptor inhibitor for 12 months to prevent myoc

102 tors, were assigned to either control group, P2Y(12) receptor inhibitor withdrawn 5 to 7 days before

103 of the combination of aspirin and a platelet P2Y(12) receptor inhibitor, has been the gold standard o

104 with stenting, treatment with aspirin and a P2Y12 receptor inhibitor also becomes indicated.

105 studies, mice were treated with the platelet P2Y12 receptor inhibitor clopidogrel or placebo.

106 by single antiplatelet therapy (SAPT) with a P2Y12 receptor inhibitor confers benefits compared with

107 t therapy (DAPT) with aspirin and a platelet P2Y12 receptor inhibitor is the standard antithrombotic

108 Ticagrelor (Brilinta), a commonly prescribed P2Y12 receptor inhibitor used after myocardial infarctio

109 sk in major bleeding by combining aspirin, a P2Y12 receptor inhibitor, and an anticoagulant.

110 me (ACS) patients are not pre-treated with a P2Y12 receptor inhibitor, and percutaneous coronary inte

111 with indications for CABG and on aspirin and P2Y(12) receptor inhibitors, were assigned to either con

112 d to treat excessive bleeding in patients on P2Y12 receptor inhibitors (RI).

113 P2Y12 receptor inhibitors clinically in use such as clop

114 after discharge for beta-blockers, platelet P2Y12 receptor inhibitors, statins, and angiotensin-conv

115 elor and prasugrel are guideline-recommended P2Y12 receptor inhibitors.

116 ess and novel platelet adenosine diphosphate P2Y12 receptor inhibitors.

117 ilar to that of rodent microglia in that the P2Y12 receptor initiates process extension.

118 Blocking P2Y12 receptor is a clinically well-validated strategy f

119 Thus, the P2Y12 receptor is required for proinflammatory actions o

120 uated by PKC inhibitors, whereas that of the P2Y12 receptor is unaffected.

121 osine diphosphate (ADP)-reactive purinergic (P2Y12) receptor is required for LTE4-mediated pulmonary

122 Because clopidogrel antagonizes the platelet P2Y12 receptor, it is widely prescribed for patients wit

123 P2X(4), P2X(5), P2X(7), P2Y(2), P2Y(11), and P2Y(12) receptors localized to the cytoplasm.

124 y rapid feedback amplification that involves P2Y(12) receptor-mediated activation of Syk.

125 nts, but had no effect on Cys17Ser/Cys270Ser P2Y(12) receptor-mediated inhibition of adenylyl cyclase

126 Ligand docking on P2Y1 and P2Y12 receptor models was guided by mutagenesis results,

127 In platelets from mice lacking the P2Y12 receptor, neither alpha-thrombin nor AYPGKF caused

128 , and/or ATP; (iii) the activation of P2X(1)/P2Y(12) receptors on adjacent PLTs; and (iv) the recursi

129 signaling, via selective stimulation of the P2Y(12) receptor or alpha(2A)-adrenergic receptor, respe

130 ntial signalling and cell activation through P2Y12 receptor or receptor heterodimers but no specific

131 The P2Y(12) receptor (P2Y(12)) plays a central role in ampli

132 The G protein-coupled, ADP-activated P2Y(12) receptor (P2Y(12)R) expressed by microglial cell

133 ding motif of the platelet G protein-coupled P2Y(12) receptor (P2Y(12)R) is required for effective re

134 A platelet ADP P2Y12 receptor (P2Y12) inhibitor plus aspirin is standar

135 The human P2Y12 receptor (P2Y12-R) is a member of the G protein co

136 P2Y12 receptor (P2Y12-R) signaling is mediated through G

137 Ticagrelor is a potent antagonist of the P2Y12 receptor (P2Y12R) and consequently an inhibitor of

138 ed BSM contraction is blocked by a selective P2Y12 receptor (P2Y12R) antagonist, PSB 0739 (25 muM), b

139 Defects of the platelet P2Y12 receptor (P2Y12R) for adenosine diphosphate (ADP)

140 Recently, the P2Y12 receptor (P2Y12R) has been identified as a promisi

141 sence of microglia or blockade of microglial P2Y12 receptor (P2Y12R) substantially impairs neurovascu

142 The P2Y12 receptor (P2Y12R), one of eight members of the P2Y

143 th tests measuring the adenosine diphosphate-P2Y12 receptor pathway, without significant variations i

144 Platelet P2Y12 receptors play a central role in the regulation of

145 elated factors (higher on-treatment platelet P2Y12 receptor reactivity and premature thienopyridine d

146 Selective blockade of the P2Y(12) receptor results in the inhibition of Syk phosph

147 Unlike AR-C 69931MX, a P2Y(12) receptor-selective antagonist, the GIRK channel

148 ene adenosine 5'-triphosphate (AR-C67085), a P2Y12 receptor-selective antagonist, and adenosine-2'-ph

149 inhibited in the presence of AR-C69931MX, a P2Y12 receptor-selective antagonist, or GF 109203X, a pr

150 or that abolishes secretion, or AR-C66096, a P2Y12 receptor-selective antagonist; alpha-thrombin-indu

151 Cloning of the P2Y12 receptor should facilitate the development of bett

152 ion symptoms, suggesting a contribution from P2Y(12) receptor signaling in this subset.

153 PMA reduced subsequent ADP-induced P2Y1 and P2Y12 receptor signaling.

154 ators is ADP, which, acting through platelet P2Y12 receptors, strongly amplifies aggregation.

155 Activation of P2Y(1) and P2Y(12) receptors, through secreted ADP that is stimulat

156 We use CD45, CD11b/c, and p2y12 receptor to identify microglia and evaluate their

157 X1, and A2b receptors was unchanged, whereas P2Y12 receptor was significantly downregulated, suggesti

158 in undergoes synergy with ADP acting via the P2Y12 receptor whereas there is no synergy via the P2Y1

159 ructed a chimeric hemagglutinin-tagged human P2Y(12) receptor with its C terminus replaced by the cor

160 tivation by blocking the type 12 purinergic (P2Y(12)) receptor, would attenuate the severity of sinon