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

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

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

9 receptors supplements signaling through the P2Y1 receptor.

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

11 and triphosphates are agonists at the human P2Y1 receptor.

12 3 and TM7 on the exofacial side of the human P2Y1 receptor.

13 enine nucleotide binding pocket of the human P2Y1 receptor.

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

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

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

17 cells stably expressing the human or turkey P2Y1 receptor.

18 ATP-derived ADP attracts astrocytes via the P2Y1 receptor.

19 1 antagonists or CRISPR-Cas9 knockout of the P2Y1 receptor.

20 response, continue to express the purinergic P2Y1 receptor.

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

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

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

24 greatly reduced the ability to interact with P2Y1 receptors.

25 rved in muscles with genetic deactivation of P2Y1 receptors.

26 purinergic neurotransmission is mediated via P2Y1 receptors.

27 ediated responses in HEK293 cells expressing P2Y1 receptors.

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

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

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

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

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

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

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

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

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

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

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

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

40 f ATP to modulate baroreflex sensitivity via P2Y(1) receptors.

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

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

43 P2Y1 receptor activation appears to be necessary and suf

44 PKC inhibitors prevented P2Y1 receptor activation of TRPV4.

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

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

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

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

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

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

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

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

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

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

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

56 hich propagates/amplifies Ca(2+) signals via P2Y(1) receptors and Ca(2+) recruitment from the intrace

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

76 ses in distal colon were blocked by MRS2500 (P2Y1 receptor antagonist), apamin (SK channel antagonist

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

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

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

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

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

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

83 gic neurotransmission in proximal colon, but P2Y1 receptor antagonists were more effective in distal

84 9-position of adenine, are moderately potent P2Y1 receptor antagonists.

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

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

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

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

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

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

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

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

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

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

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

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

97 As a result, activation of P2Y1 receptors by PolyP reduced calcium signal acting th

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

99 The P2Y1 receptor couples to Gq and mobilizes intracellular

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

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

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

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

104 versible and associated with purinergic type P2Y1 receptor desensitization.

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

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

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

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

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

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

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

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

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

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

115 gonists of TRPV4 channels; (3) antagonist of P2Y(1) receptors for ATP; and (4) inhibitors of phosphol

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

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

118 Recent studies of P2Y(1) receptor function in seizures and epilepsy have p

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

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

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

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

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

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

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

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

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

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

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

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

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

132 ATP in turn stimulates P2Y1 receptors in neurons.

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

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

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

136 gain by 40% (p = 0.031), whereas blockade of P2Y(1) receptors increased baroreflex gain by 57% (p = 0

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

157 P2Y1 receptor-mediated responses were enhanced in TRPV4-

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

159 e mice, we demonstrate that the metabotropic P2Y(1) receptor mediates either proconvulsive or anticon

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

161 Stimulation of P2Y1 receptors modulates the amplitudes of STHs.

162 kedly decreased expression of the purinergic P2Y1 receptor mRNA.

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

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

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

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

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

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

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

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

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

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

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

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

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

176 docking analysis on the crystal structure of P2Y(1) receptor (P2Y(1)R) with 923 derivatives of 1-indo

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

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

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

180 P2Y1 receptor (P2Y1R) structures showed two antagonists

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

182 1 glutamate mGluR5 receptors and nucleotide P2Y1 receptors (P2Y1Rs) show promiscuous ion channel cou

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

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

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

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

187 by astrocytes via activation of metabotropic P2Y(1) receptors, recruitment of phospholipase C, releas

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

218 ]2MeS-ADP to P2Y(12), whereas binding to the P2Y(1) receptor was normal.

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

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

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

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

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

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

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

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

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

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

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

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

231 Platelet-derived ADP/ATP and MC-associated P2Y(1) receptors were essential.

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

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

234 P2Y1 receptors were found in fetal keratinocytes positiv

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

236 P2Y1 receptors were only expressed in the stroma surroun

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

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

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

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

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

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

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