ライフサイエンスコーパス: P2Y(1) receptor

1 fused mice (all inactive at the vasodilatory P2Y(1) receptor).

2 se agonists in platelets from mice that lack P2Y1 receptor.

3 d P2Y12 receptor and the G(alpha)(q)-coupled P2Y1 receptor.

4 reatly reduced the antagonist potency at the P2Y1 receptor.

5 e, and that this response is mediated by the P2Y1 receptor.

6 ted to act as competitive antagonists at the P2Y1 receptor.

7 ect on the capacity of MRS 2179 to block the P2Y1 receptor.

8 receptors supplements signaling through the P2Y1 receptor.

9 kidney 293 cells, which natively express the P2Y1 receptor.

10 and triphosphates are agonists at the human P2Y1 receptor.

11 3 and TM7 on the exofacial side of the human P2Y1 receptor.

12 enine nucleotide binding pocket of the human P2Y1 receptor.

13 ant modulatory role in ligand binding to the P2Y1 receptor.

14 urkey P2Y1 receptor and -36 mV for the human P2Y1 receptor.

15 were devoid of agonist activity at the human P2Y1 receptor.

16 cells stably expressing the human or turkey P2Y1 receptor.

17 response, continue to express the purinergic P2Y1 receptor.

18 ion of the genes encoding E-NTPDase2 and the P2Y1 receptor.

19 created based on the X-ray structures of the P2Y1 receptor.

20 at alpha,beta-methylene-ADP is an agonist at p2y1 receptors.

21 rved in muscles with genetic deactivation of P2Y1 receptors.

22 greatly reduced the ability to interact with P2Y1 receptors.

23 purinergic neurotransmission is mediated via P2Y1 receptors.

24 in ventilation is mediated by ATP acting at P2Y1 receptors.

25 ediated responses in HEK293 cells expressing P2Y1 receptors.

26 dent manner, whereas it had no effect on the P2Y(1) receptor.

27 P) signaling through the P2Y(12) and not the P2Y(1) receptor.

28 ps greatly reduced antagonist potency at the P2Y(1) receptor.

29 coat; this action of ATP is mediated by the P2Y(1) receptor.

30 ith intestinal secretory glands, express the P2Y(1) receptor.

31 -O-(2-thiodiphosphate) for activation of the P2Y(1) receptor.

32 rough the cooperation of H1 and P2 (probably P2Y1) receptors.

33 less well, exhibiting micromolar affinity at P2Y(1) receptors.

34 ing human B(1)-bradykinin or truncated human P2Y(1) receptors.

35 formation, which greatly enhanced potency at P2Y(1) receptors.

36 were also highly selective, full agonists at P2Y(1) receptors.

37 ion appeared to be favored in recognition at P2Y(1) receptors.

38 s, NHERF binds to the tail of the purinergic P2Y1 receptor, a seven-transmembrane receptor with an in

39 et aggregation in combination with selective P2Y(1) receptor activation.

40 P2Y1 receptor activation appears to be necessary and suf

41 PKC inhibitors prevented P2Y1 receptor activation of TRPV4.

42 The potent P2Y1 receptor agonist 2-methylthio-ATP (2-MeSATP) had no

43 P2Y2 receptor agonist UTP (p<0.001), and the P2Y1 receptor agonist 2MeSADP (p<0.05).

44 knockdown is refractory to activation by the P2Y1 receptor agonist ATP and shows aberrant purinergic

45 nce of NTPDase2 than in cells expressing the P2Y(1) receptor alone.

46 ration-dependent manner, indicating that the P2Y1 receptor alone mediates ADP-induced generation of t

47 not essential for recognition by the turkey P2Y(1) receptor, although a cyclic structure appears to

48 ytoma cells expressing the recombinant human P2Y(1) receptor and by using the radiolabeled antagonist

49 Similar effects were observed when the P2Y(1) receptor and NTPDase1 were expressed on different

50 replaced by the corresponding part of human P2Y(1) receptor and stably expressed it in Chinese hamst

51 tor, confirming the crucial role of platelet P2Y(1) receptor and subsequent activation of RhoA.

52 acid gene product with 61-64% similarity to P2Y(1) receptors and 21-37% similarity to other P2Y rece

53 reversal potential of -38 mV for the turkey P2Y1 receptor and -36 mV for the human P2Y1 receptor.

54 n identified as selective antagonists at the P2Y1 receptor and have been modified structurally to inc

55 , we conclude that ADP activates nPKCeta via P2Y1 receptor and is subsequently dephosphorylated by PP

56 adenosine 5'-triphosphate (ATP), binding to P2Y1 receptors and activating small conductance K(+) cha

57 dy provides a link between purine binding to P2Y1 receptors and activation of SK3 channels in PDGFRal

58 onto receptor (type II) cells by activating P2Y1 receptors and enhancing ATP secretion.

59 owed high levels of expression of purinergic P2Y1 receptors and SK3 K(+) channels in PDGFRalpha(+) ce

60 irway epithelial cells, which also express a P2Y(1) receptor, and that the P2Y(2)-R is the sole purin

61 (2)-R(-/-) cells, which was inhibited by the P2Y(1) receptor antagonist adenosine 3'-5'-diphosphate.

62 xyadenosine bisphosphate analogue was a pure P2Y(1) receptor antagonist and equipotent to the ribose

63 signaling was significantly inhibited by the P2Y(1) receptor antagonist MRS 2179 or by knockdown of P

64 ked by MK-801, by the ATPase apyrase, by the P2Y(1) receptor antagonist MRS2179 and by depletion of i

65 The P2Y(1) receptor antagonist MRS2179 slowed propulsive mot

66 to ADPR, but not ADP, were inhibited by the P2Y1 receptor antagonist (1R,2S,4S,5S)-4-[2-iodo-6-(meth

67 The present study used the selective P2Y1 receptor antagonist MRS2500 (1 mum) and the nitric

68 completely absent in P2ry1(-/-) mice and the P2Y1 receptor antagonist MRS2500 had no effect on electr

69 l firing, an effect blocked by the selective P2Y1 receptor antagonist MRS2500.

70 didate from our in vitro screen (MRS 2179, a P2Y1 receptor antagonist) also improves histological and

71 ut not by AMP, and was inhibited by MRS2179 (P2Y1 receptor antagonist) but not by AR-C69931MX (P2Y12/

72 d its metabolite, ADP, whereas the selective P2Y1 receptor antagonist, MRS2179, partially attenuated

73 Pretreatment of platelets with MRS-2179, a P2Y1 receptor antagonist, or YM-254890, a G(q) blocker,

74 onships of adenosine-3', 5'-bisphosphates as P2Y(1) receptor antagonists have been explored, revealin

75 ublication, we have characterized the SAR as P2Y(1) receptor antagonists of acyclic analogues of aden

76 cture-activity of adenosine bisphosphates as P2Y1 receptor antagonists and have led to the identifica

77 osition of the adenine ring were more potent P2Y1 receptor antagonists than analogues containing vari

78 9-position of adenine, are moderately potent P2Y1 receptor antagonists.

79 lular space and the activation of peripheral P2Y1 receptors appear to participate in the generation o

80 P2Y(1) receptors are activated by ADP and occur on endot

81 We also identify that P2X(1), P2X(7), and P2Y(1) receptors are involved in viral replication.

82 ly, the results have indicated that although P2Y1 receptors are involved in the initiation of platele

83 beta-NAD is an agonist for P2Y1 receptors, as demonstrated by receptor-mediated res

84 Tail current analysis of the novel P2Y1 receptor-associated cation conductance revealed tha

85 In conclusion, as for P2Y(1) receptors, at least three adenosine receptors fav

86 ere specific for the phospholipase C-coupled P2Y1 receptor, because no agonistic or antagonistic effe

87 ding to at least two distinct domains of the P2Y1 receptor, both outside and within the TM core.

88 sed cell size and the number of cell surface P2Y(1) receptors, but not P2Y(1) receptor density.

89 cribe specific competitive antagonism of the P2Y1 receptor by an adenine nucleotide derivative and pr

90 In addition, genetic knockdown of the P2Y1 receptor by in vivo application of short hairpin RN

91 drolysable ADP analogue, ADPbetaS, acting at P2Y1 receptors, caused robust local and spreading dilata

92 The P2Y1 receptor couples to Gq and mobilizes intracellular

93 ted from these mice did not exhibit a higher P2Y(1) receptor density or increased reactivity to ADP.

94 er of cell surface P2Y(1) receptors, but not P2Y(1) receptor density.

95 migration in vitro were exclusively platelet P2Y(1) receptor dependent.

96 or, the presence of the NTPDase2 resulted in P2Y(1) receptor-dependent increases in basal activity.

97 versible and associated with purinergic type P2Y1 receptor desensitization.

98 ctivation of the novel cation current by the P2Y1 receptor does not involve a G protein.

99 These results indicate that the P2Y1 receptor exhibits both metabotropic properties and

100 ere weak antagonists in studies of the human P2Y1 receptor expressed in human Jurkat cells.

101 We also examine the possible contribution of P2Y1 receptors expressed in the RTN to the purinergic dr

102 ither in the same cell as the receptor or in P2Y(1) receptor-expressing cells cocultured with NTPDase

103 e might explain this discrepancy of results, P2Y1 receptor-expressing 1321N1 cells were incubated for

104 e in Cl- current similar to that observed in P2Y1 receptor-expressing oocytes but had no effect on ca

105 d both the cation current and Cl- current in P2Y1 receptor-expressing oocytes with EC50 values and an

106 Thus, the enhancement of P2Y(1) receptor expression induced by Mpl ligand in mega

107 tol phosphate levels occurred with wild-type P2Y(1) receptor expression, levels in cells expressing t

108 responses activated by the G protein-coupled P2Y1 receptor for ADP.

109 ort the cloning of a cDNA clone encoding the P2Y1 receptor from a human platelet cDNA library by homo

110 r) is involved in this pathway, and that the P2Y(1) receptor (G(q)-coupled ADP receptor) may play a l

111 Costimulation of P2X1 and P2Y1 receptors generated a superadditive Ca(2+) increase

112 in the extracellular loops (EL) of the human P2Y1 receptor has been investigated.

113 nosine 5'-diphosphate (2-MeSADP) was lost in P2Y1 receptors having F226A, K280A, or Q307A mutations,

114 cation of the C-terminal region of the human P2Y(1) receptor identified a short region responsible fo

115 signaling responses, we engineered the human P2Y(1) receptor in a fusion protein with a member of the

116 he antiserum specifically detected the human P2Y(1) receptor in transfected 1321N1 cells.

117 ging evidence for significant involvement of P2Y(1) receptors in local enteric neural control and coo

118 These results demonstrate the role of the P2Y1 receptor in ADP-induced platelet shape change and c

119 specific upregulation of the ADP-responsive P2Y1 receptor in the DRGs.

120 Inhibition of the P2Y1 receptor in the RTN had no effect on CO2 responsivn

121 Conversely, exogenous expression of P2Y1 receptors in Cx43-null cells restored their migrati

122 munication attributable to reduced levels of P2Y1 receptors in neural progenitor cells lacking Cx43 a

123 ATP in turn stimulates P2Y1 receptors in neurons.

124 that purines activate SK currents via mainly P2Y1 receptors in PDGFRalpha(+) cells.

125 The activation of P2Y1 receptors in platelets contributes to platelet aggr

126 Unilateral blockade of P2Y1 receptors in the preBotC via local antagonist injec

127 A new rhodopsin-based molecular model of the P2Y1 receptor indicated that the optimal docked orientat

128 three extracellular loops (ELs) of the human P2Y1 receptor indicates the existence of two essential d

129 icroM ADP in rat platelets and inhibition of P2Y(1) receptor-induced phospholipase C (PLC) activity p

130 We now report that activation of endogenous P2Y1 receptors induces inhibition of the M-current in ra

131 DP were blocked by 500 nmMRS2179, a specific P2Y(1) receptor inhibitor, suggesting that ATP acts on P

132 important than the alpha-phosphate in ligand/P2Y1 receptor interactions.

133 ADP-induced P2Y1 receptor internalization is attenuated by PKC inhib

134 e results suggest that basal activity of the P2Y(1) receptor is maintained by paracrine or autocrine

135 The P2Y(1) receptor is responsible for the initiation of pla

136 The P2Y1 receptor is a G protein-coupled receptor (GPCR) and

137 The P2Y1 receptor is a membrane-bound G protein-coupled rece

138 The P2Y1 receptor is present in the heart, in skeletal and v

139 racellular signaling from both the P2TAC and P2Y1 receptors is essential for ADP-induced platelet agg

140 ndicating that coactivation of the P2Y12 and P2Y1 receptors is essential for this event.

141 a to purinergic agents demonstrated that the P2Y1 receptor-mediated increase in fictive inspiratory f

142 of excitability are caused, respectively, by P2Y1 receptor-mediated inhibition of a two-pore domain p

143 man endothelial cell migration by activating P2Y1 receptor-mediated MAPK pathways, possibly contribut

144 We performed a screen for P2Y1 receptor-mediated receptor tyrosine kinase transact

145 that ATP excitation of the preBotC involves P2Y1 receptor-mediated release of Ca(2+) from intracellu

146 Our observation that P2Y1 receptor-mediated responses involve Flt3 transactiv

147 P2Y1 receptor-mediated responses were enhanced in TRPV4-

148 Platelet P2X1 receptor-, but not P2Y1 receptor-, mediated increases in intracellular calc

149 tive binding site of the previously reported P2Y(1) receptor model.

150 Stimulation of P2Y1 receptors modulates the amplitudes of STHs.

151 kedly decreased expression of the purinergic P2Y1 receptor mRNA.

152 jection of Mpl ligand into mice up-regulated P2Y(1) receptor mRNAs in megakaryocytes, as shown by in

153 expressing either wild-type NTPDase1 or the P2Y(1) receptor-NTPDase1 fusion protein exhibited nucleo

154 ly normal receptor signaling activity of the P2Y(1) receptor-NTPDase1 fusion protein, we quantitated

155 is related to the evolutionary forerunner of P2Y(1) receptors of higher organisms.

156 r antagonists at the phospholipase C-coupled P2Y1 receptor of turkey erythrocytes, at recombinant hum

157 The molecular basis for recognition by human P2Y1 receptors of the novel, competitive antagonist 2'-d

158 Expression of pannexin-1 and ADP-sensitive P2Y1 receptor on human subcutaneous fibroblasts was conf

159 The P2Y1 receptor on the neurones was identified as a metabo

160 presence of functional M-current-inhibitory P2Y1 receptors on hippocampal pyramidal neurons, as pred

161 eBotC astrocytes during hypoxia and acts via P2Y1 receptors on inspiratory neurons (and/or glia) to e

162 mediated by release of ATP and its action at P2Y1 receptors on morphologically identified neurones in

163 cells stably expressing either the wild-type P2Y(1) receptor or the fusion protein.

164 receptor whereas there is no synergy via the P2Y1 receptor or with thromboxanes.

165 as a selective high-affinity, non-nucleotide P2Y(1) receptor (P2Y1-R) antagonist.

166 The human P2Y1 receptor (P2Y1-R) was purified after high-level exp

167 In response to adenosine 5'-diphosphate, the P2Y1 receptor (P2Y1R) facilitates platelet aggregation,

168 P2Y1 receptor (P2Y1R) structures showed two antagonists

169 rgic motor neurotransmission, acting through P2Y1 receptors (P2Y1R), mediates inhibitory neural contr

170 1 glutamate mGluR5 receptors and nucleotide P2Y1 receptors (P2Y1Rs) show promiscuous ion channel cou

171 flux stimulation) and at turkey erythrocyte P2Y1 receptors (phospholipase C activation).

172 e two disulfide bridges present in the human P2Y1 receptor play a major role in the structure and sta

173 ions (M-SMP) of rat colon was reduced by the P2Y1 receptor (R) antagonist 2'deoxy-N6-methyl adenosine

174 ate > or = 5'uridine-diphosphate, supports a P2Y1 receptor (R).

175 receptor apparently depends on the degree of P2Y1 receptor reserve.

176 Coexpression of NTPDase1 with the P2Y(1) receptor resulted in increases in the EC(50) for

177 On the other hand, the P2Y1 receptor selective antagonist, adenosine-2'-phospha

178 might act to trigger eye development through P2Y1 receptors, selective in Xenopus for ADP, we simulta

179 alcium flux that was completely blocked by a P2Y1 receptor-selective antagonist and was not cross-des

180 and shape change were unaffected by A3P5P, a P2Y1 receptor-selective antagonist, and/or cyproheptadin

181 enosine-2'-phosphate-5'-phosphate (A2P5P), a P2Y1 receptor-selective antagonist, inhibited ADP-induce

182 tive P2 receptor antagonist, and MRS-2179, a P2Y1 receptor-selective antagonist, reduced the prolifer

183 he receptors themselves or steps in the post-P2Y(1) receptor signal transduction cascade might be pot

184 cells revealed that both isoforms regulated P2Y1 receptor signaling and trafficking, although only P

185 selective agonists, and was blocked by three P2Y(1)-receptor-specific antagonists.

186 L 66096, but not by alpha, beta-MeATP or the P2Y1 receptor-specific antagonists, A3P5PS, A3P5P, or A2

187 ular calcium increases were inhibited by the P2Y1 receptor-specific antagonists, adenosine 3'-phospha

188 antagonists in studies with the cloned human P2Y1 receptor stably expressed in 1321N1 human astrocyto

189 d triphosphates was determined for the human P2Y1 receptor stably expressed in human 1321N1 astrocyto

190 P2Y(1) receptor stimulation with 2-methylthio ADP (2-MeS

191 widespread and abundant distribution of the P2Y(1) receptor suggests its involvement in a number of

192 f the analogues were more potent at P2X7 and P2Y1 receptors than 2, which acted in the micromolar ran

193 of NTPDase1 decreased basal activity of the P2Y(1) receptor, the presence of the NTPDase2 resulted i

194 lic and acyclic) bisphosphate antagonists of P2Y(1) receptors, there was a significant correlation be

195 ically through interaction with the RAGE and P2Y1 receptors, thereby eliciting intracellular Ca(2+) r

196 Immunofluorescence localized the P2Y(1) receptor to the brush border membrane of duodenal

197 eptor inhibitor, suggesting that ATP acts on P2Y(1) receptors to inhibit chloride channels.

198 Synaptically released ATP acts at these P2Y(1) receptors to stimulate glandular secretion of ele

199 s, is required for proper trafficking of the P2Y1 receptor to the cell surface.

200 e determine coupling of mGluR5 receptors and P2Y1 receptors to calcium channels.

201 spiratory rhythm-generating network acts via P2Y1 receptors to mediate this effect.

202 ion, release a gliotransmitter that acts via P2Y1 receptors to stimulate ventilation and reduce the s

203 Specifically, the binding site of the P2Y(1) receptor was found to be sufficiently accommodati

204 he regional and cellular distribution of the P2Y(1) receptor was investigated in the human brain by u

205 ]2MeS-ADP to P2Y(12), whereas binding to the P2Y(1) receptor was normal.

206 Expression of the P2Y(1) receptor was not detected in other non-neuronal c

207 At the cellular level, the P2Y(1) receptor was strikingly localised to neuronal str

208 Activation of the human P2Y(1) receptor was studied in the presence of NTPDase1

209 The biological activity of each analogue at P2Y(1) receptors was characterized by measuring its capa

210 nucleotide 3',5'-bisphosphate antagonists of P2Y(1) receptors was established by using a ring-constra

211 In stark contrast, activation of P2Y(1) receptors was ineffective in this regard.

212 first on activated satellite cells, and the P2Y1 receptor was also expressed on infiltrating immune

213 A computer-generated model of the human P2Y1 receptor was built and analyzed to help interpret t

214 The activity of each analogue at P2Y1 receptors was determined by measuring its capacity

215 The activity of each analogue at P2Y1 receptors was determined by measuring its capacity

216 The potency of nucleotide antagonists at P2Y1 receptors was enhanced by replacing the ribose moie

217 Strong immunostaining for P2Y1 receptors was shown in most cells in these cultures

218 nctional properties of the G protein-coupled P2Y1 receptor were investigated in Xenopus oocytes.

219 The P2X5 and P2Y1 receptors were expressed first on activated satelli

220 P2Y1 receptors were found in fetal keratinocytes positiv

221 distinct zones of the developing epidermis: P2Y1 receptors were found in the basal layer, P2X5 recep

222 P2Y1 receptors were only expressed in the stroma surroun

223 These results indicate that, unlike the P2Y(1) receptor, which has 2 essential disulfide bridges

224 Surprisingly, BzATP binds the P2Y(1) receptor, which is primarily responsible for the

225 ll agonists exhibiting micromolar potency at P2Y(1) receptors, while the corresponding ribosides were

226 osphate moiety, was a full antagonist at the P2Y(1) receptor with an IC(50) value of 1.60 micro inver

227 ocytes expressing either the human or turkey P2Y1 receptor with adenine nucleotide agonists resulted

228 phosphate) (7), was a full antagonist at the P2Y1 receptor with an IC(50) value of 0.48 microM.

229 the most potent antagonist selective for the P2Y(1) receptor yet reported.