ライフサイエンスコーパス: CRTH2

1 ) and PGD2 receptor 2 (DP2, sometimes termed CRTH2).

2 -homologous molecule expressed on Th2 cells (CRTH2).

3 receptor homologous molecule on T(H)2 cells (CRTH2).

4 further investigate the in vivo function of CRTH2.

5 ant receptors such as CCR4, CCR5, CXCR6, and CRTH2.

6 ion of CXCR3 and down-regulation of CCR4 and CRTH2.

7 le dual antagonist of human D-prostanoid and CRTH2.

8 y for the human, monkey, dog, rat, and mouse CRTH2, 2) interacts with CRTH2 in a reversible manner, 3

9 st on recombinant and endogenously expressed CRTH2, 5) demonstrates good oral bioavailability and met

10 Receptor Homologous to the T helper 2 cell (CRTH2), a G protein-coupled receptor, present on a subse

11 -homologous molecule expressed on TH2 cells (CRTH2), a receptor for prostaglandin D(2) (PGD(2)), is e

12 ith amniocytes and myocytes transfected with CRTH2 acting as a positive control in flow cytometry stu

13 eptors to amplify the biological response to CRTH2 activation.

14 This effect was mimicked by the selective CRTH2 agonist 13,14-dihydro-15-keto-PGD(2), inhibited by

15 effect of PGD2 was mimicked by the selective CRTH2 agonist 13,14-dihydro-15-keto-PGD2 but not by the

16 The CRTH2 agonist had no effect on NF-kappaB activity in amn

17 The effect of a small molecule CRTH2 agonist on NF-kappaB activity in human cultured am

18 ILC2 activation through CRTH2 also upregulated the expression of IL-33 and IL-25

19 oteins abolishes the Ca(2+) response to both CRTH2 and DP agonists, whereas inhibition of Galpha(i) p

20 We show that CRTH2 and DP receptors modulate one another's signaling

21 The cross-talk of CRTH2 and DP receptors was investigated by using both a

22 on of the profibrotic BRP-39 receptor Ptgdr2/Crth2 and expression of the profibrotic markers Lgals3,

23 d hyper-activated through the interaction of CRTH2 and NKp30 with elevated tumour-derived PGD2 and B7

24 ggesting that the stimulation is mediated by CRTH2 and not DP.

25 rs533116 and allergic asthma, expression of CRTh2 and Th2 cytokine production.

26 -homologous molecule expressed on Th2 cells (CRTH2) and has been detected at high concentrations at s

27 ogous molecule expressed on TH2 lymphocytes (CRTH2) and PGD(2) receptor 1 (DP1).

28 omologous molecule expressed on T(H)2 cells (CRTH2), and D-type prostanoid (DP) receptor.

29 ogous molecule expressed on Th2 lymphocytes (CRTh2), and phosphodiesterase (PDE)-4 inhibitors.

30 between vasoactive intestinal peptide (VIP), CRTH2, and eosinophil recruitment.

31 as well as X-hydroxy-naphthoyl analogues of CRTh2 antagonist 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro

32 erein we describe the discovery of the novel CRTh2 antagonist 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro

33 d on the discovery of the recently disclosed CRTh2 antagonist 2-(2-benzoyl-3,4-dihydro-1H-pyrido[4,3-

34 OC000459 is a selective CRTH2 antagonist and would be expected to suppress eosin

35 estigate the efficacy and safety of the oral CRTH2 antagonist BI 671800 (50, 200, and 400 mg twice da

36 The CRTH2 antagonist CAY10595 improved, whereas the DP antag

37 Slow CRTh2 antagonist dissociation could provide increased re

38 The CRTH2 antagonist OC000459 has previously been demonstrat

39 The CRTH2 antagonist OC000459 has previously been demonstrat

40 inhibited phospho-65 in PBMC'S, however the CRTH2 antagonist was not able to attenuate this effect.

41 -yl}acetic acid (MK-7246), a novel synthetic CRTH2 antagonist.

42 ctivated human mast cells and inhibited by a CRTH2 antagonist.

43 (1), a diazine indole acetic acid containing CRTH2 antagonist.

44 C50 = 6 nM), selective, and orally available CRTh2 antagonist.

45 An 8-week treatment with the CRTH2-antagonist, OC000459, exerts modest, but significa

46 ation and highlight the potential utility of CRTH2 antagonists in the treatment of allergic diseases.

47 ,14-dihydro-15-keto-PGD(2), inhibited by the CRTH2 antagonists ramatroban and TM30089, and not observ

48 All CRTh2 antagonists tested inhibited PGD2-stimulated human

49 3-acetic acids that are potent and selective CRTH2 antagonists that possess good oral bioavailability

50 New classes of CRTH2 antagonists, the pyridazine linker containing indo

51 omologous molecule expressed on T(H)2 cells (CRTH2) are implicated in asthma pathogenesis.

52 ls expressing the prostaglandin D2 receptor (CRTH2) are TH2 central memory T cells, characterized by

53 Similarly, there were lower proportions of CRTh2(+) basophils expressing surface CD203c(bright) (al

54 Proportions of allergen-stimulated DAO(+)CRTh2(+) basophils were higher in participants in the SC

55 evaluate the structural features that confer CRTH2 binding selectivity, structure-activity relationsh

56 contribute to adaptive type 2 immunity; thus CRTH2 bridges the innate and adaptive pathways in human

57 th more eosinophils and higher expression of CRTh2 by both CD4(+) T cells and eosinophils (P < 0.05).

58 In addition to PGD2, CRTH2 can be activated by indomethacin, a nonselective c

59 lls (ILC2) include IL-5- and IL-13-producing CRTh2(+)CD127(+)cells that are implicated in early prote

60 Infiltrated CRTH2+CD4+ TH2 effector memory T cells in skin lesion of

61 CRTH2+CD4+ TH2 memory cells activated by TSLP-DCs underg

62 etin (TSLP) can induce a robust expansion of CRTH2+CD4+ TH2 memory cells, while maintaining their cen

63 e was associated with a higher proportion of CRTh2(+) cells during Th2 differentiation as well as mor

64 in effector memory CD4 T cells that include CRTH2(+) cells through IL-4 and TCR-independent pathways

65 ypic ILC2 characteristics, lineage(-)CD127(+)CRTH2(+) cells, responded to IL-33 and produced large qu

66 subjects, the peanut-specific Th2 (CD154(+) CRTh2(+) ) cells expressed more CD200R than the non-alle

67 than the non-allergen-specific Th2 (CD154(-) CRTh2(+) ) cells.

68 CRTh2 (chemoattractant-receptor homologous molecule expr

69 kine production in human Th2 cells through a CRTH2-dependent mechanism in the absence of any other co

70 Therefore the CRTH2/DP heteromer might not only represent a functional

71 one another's signaling properties and form CRTH2/DP heteromers without altering their ligand-bindin

72 We investigated DP and CRTH2 expression and function during human and murine ul

73 It is shown that CRTH2 expression by eosinophils from allergic rhinitis (

74 DP and CRTH2 expression changed in leukocytes of patients with

75 Endogenous CRTH2 expression in amniocytes, myocytes and peripheral

76 ous molecule expressed on T(H)2 lymphocytes (CRTH2) expression and T(H)2 cytokine production--are spe

77 ometry regarding levels of CD23, CD44, CD54, CRTH2, FOXP3, and galectin-10.

78 molecule expressed on T(H)2 cells-positive (CRTH2(+)), hematopoietic prostaglandin D synthase-positi

79 Although subsets of human CRTh2(+)ILC2 differentially express CD117 (c-kit recepto

80 dog, rat, and mouse CRTH2, 2) interacts with CRTH2 in a reversible manner, 3) exhibits high selectivi

81 e sought to determine the role of PGD(2) and CRTH2 in human ILC2s and compare it with that of the est

82 In this study we show a novel function of CRTH2 in mediating an inhibitory effect of PGD(2) on the

83 The cellular distribution of CRTH2 in non-immune cells has not been extensively resea

84 nt study was to determine the involvement of CRTH2 in promoting nasal and ocular symptoms in allergic

85 irst evidence of association between VIP and CRTH2 in recruiting eosinophils.

86 However, the function of CRTH2 in these cells is unclear.

87 PGD(2) binding to CRTH2 induced ILC2 migration and production of type 2 cy

88 We find that the DP receptor amplifies the CRTH2-induced Ca(2+) release from intracellular stores a

89 However, CRTH2 internalization occurs independently of the DP rec

90 CRTH2 internalized upon treatment with PGD2 and 11-dehyd

91 CRTH2 is a G-protein-coupled receptor that mediates the

92 ory function of CRTH2 is well recognized and CRTH2 is hence considered an important emerging pharmaco

93 In conclusion, CRTH2 is not expressed on human amniocytes or myocytes a

94 on blood leukocytes is downregulated in UC, CRTH2 is present in colon tissue, where it may contribut

95 Although the proinflammatory function of CRTH2 is well recognized and CRTH2 is hence considered a

96 molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor that has been rep

97 -homologous molecule expressed on Th2 cells (CRTH2) is a G protein-coupled receptor that mediates the

98 t receptor-homologous molecule on Th2 cells (CRTH2) is a prostaglandin D(2) (PGD(2)) receptor, expres

99 homologous molecule expressed on Th2 cells (CRTH2), is less well defined.

100 The PGD2 receptor, CRTH2, is expressed on basophils, eosinophils, and Th2 l

101 is may be mediated by elevated expression of CRTh2, leading to higher numbers of circulating eosinoph

102 re associated with higher PGD(2), HPGDS, and CRTH2 levels.

103 o investigate the structural determinants of CRTH2 ligand binding, we performed site-directed mutagen

104 e exploited for the development of selective CRTH2 ligands.

105 Western blot demonstrated a novel CRTH2-mediated cytosol-to-membrane translocation of PKC-

106 alpha(i) proteins selectively attenuates the CRTH2-mediated response but not the DP signal.

107 acologic blockade of the DP receptor hinders CRTH2-mediated signal transduction.

108 CRTH2 mediates activation of Th2 cells, eosinophils and

109 ortant and potent activator of ILC2s through CRTH2 mediating strong proallergic inflammatory response

110 and co-localization between VIP peptide and CRTH2 molecules.

111 CRTH2 mRNA and IHC values were highest in patients with

112 Although CRTH2 mRNA was detected in amniocytes and myocytes, CRTH

113 ramatroban and TM30089, and not observed in CRTH2-negative T cells.

114 The decrease of CRTH2 on blood eosinophils clearly correlated with disea

115 Although expression of CRTH2 on blood leukocytes is downregulated in UC, CRTH2

116 nimal species, 6) yields ex vivo blockade of CRTH2 on eosinophils in monkeys and sheep, and 7) signif

117 with PGD(2), illustrating that activation of CRTH2 only inhibits apoptosis induced by cytokine depriv

118 higher expression of the TH2 surface marker CRTH2 (P = .04) and lower expression of the TH1 marker C

119 DP and CRTH2 play differential roles in UC.

120 this study we explored the possibility that CRTH2 plays a role in 15dPGJ2-mediated inhibition of NF-

121 ogous molecule expressed on TH2 lymphocytes (CRTh2)-positive basophils were measured by means of flow

122 psies of UC patients revealed an increase of CRTH2-positive cells in the colonic mucosa and high CRTH

123 s model of AR and suggest that antagonism of CRTH2 prevents the development of both the EPR and LPR a

124 homologous molecule expressed on Th2 cells (CRTH2) promotes chemotaxis and proinflammatory cytokine

125 ositive cells in the colonic mucosa and high CRTH2 protein content.

126 Lower CCR5/CRTH2 ratios were strongly associated with a lower value

127 QAW039 displayed high affinity for the human CRTh2 receptor (1.14 +/- 0.44 nM) expressed in Chinese h

128 Prostaglandin D2 (PGD2) acting at the CRTH2 receptor (chemoattractant receptor-homologous mole

129 irac displaced [3H]PGD2 binding at the mouse CRTH2 receptor (mCRTH2) with comparable affinity (Ki = 1

130 Treatment with the CRTH2 receptor antagonist prevented the decreases in RF

131 ut affecting endogenous PGD(2) production or CRTH2 receptor expression.

132 analysis of arylacetic acid class NSAIDs as CRTH2 receptor ligands was performed.

133 The CRTH2 receptor shares greatest sequence similarity with

134 e of its relatively slower off rate from the CRTh2 receptor.

135 nts and Eol-1 cells was mediated through the CRTH2 receptor.

136 relatively slow dissociation from the human CRTh2 receptor.

137 gous molecules expressed on T-helper type 2 (CRTh2) receptor antagonists, including fevipiprant (NVP-

138 -homologous molecule expressed on Th2 cells (CRTH2) receptor, a G protein-coupled receptor that media

139 dy provides the first clinical evidence that CRTH2 receptors contribute to airflow limitation, sympto

140 ceptor-like molecule expressed on Th2 cells (CRTH2) receptors.

141 Single nucleotide polymorphisms (SNPs) in CRTh2 (rs11571288, rs545659, rs634681) have been associa

142 These findings show an association between CRTh2 rs533116 and allergic asthma and suggest this may

143 Here, we assessed the association between CRTh2 rs533116 and allergic asthma, expression of CRTh2

144 CRTh2 rs533116 was associated with allergic asthma in Wh

145 CRTh2 rs533116 was genotyped in an ethnically diverse po

146 s assessed by stimulating Th2 cells with the CRTh2-specific agonist 13,14-dihydro-15-keto-PGD(2) (DK-

147 The ratio between CCR5 and CRTH2 T cell frequencies was used to quantify type 1 (hi

148 acity (DLCO) was associated with higher CCR5/CRTH2 T cell ratios (Th1/Tc1) (P=0.009), while in those

149 Patients with SSc exhibited lower CCR5/CRTH2 T cell ratios than those exhibited by control subj

150 Markedly reduced CCR5/CRTH2 T cell ratios were observed in SSc patients with I

151 IL-4 enhances the generation of CCR4(+) and CRTH2(+) T cells, and suppresses the generation of CXCR3

152 SP-D suppressed allergen-driven CD27(-)CD4(+)CRTh2(+) T-cell proliferation (P < 0.01), IL-4, and IL-5

153 Along with increased IL-4 and GATA-3, CRTH2(+) Th cells isolated from Th2-skewed cultures or t

154 Tc1-specific), and prostaglandin D2 receptor CRTH2 (Th2/Tc2-specific).

155 pressed CD44 and a larger fraction expressed CRTH2 than the controls.

156 tibodies (mAbs) against the PGD(2) receptor, CRTH2, the best selective Th2-cell surface marker to dat

157 Ramatroban, a dual CRTH2/thromboxane-like prostanoid receptor antagonist, m

158 In contrast, CRTH2 was decreased in eosinophils, NK, and CD3(+) T cel

159 The proportion of cells expressing CRTh2 was determined in peripheral blood from subjects w

160 of the 2 inflammatory cell receptors DP1 and CRTH2 was evaluated on luminal cells.

161 67 [1.09-6.55], P < 0.05), and expression of CRTh2 was higher in subjects with allergic airways disea

162 RNA was detected in amniocytes and myocytes, CRTH2 was not detectable at the protein level, as demons

163 interactions between CHI3L1 and the receptor CRTH2, which trafficked normally in BLOC-3 mutant HPS.