ライフサイエンスコーパス: pregnane

1 ha)-3-hydroxy-2-(2,2-dimethyl-4-morpholinyl)-pregnane-11,20-dione (19) and (2 beta,3 alpha,5 alpha)-2

2 The neurosteroid, 3alpha-hydroxy-5alpha-pregnane-20-one (1-10 microM) exhibited weak potency in

3 nt of the neurosteroid 3alpha-hydroxy-5alpha-pregnane-20-one (3alpha5alpha-ALLO) without altering the

4 he neuroactive steroid 3alpha-hydroxy-5alpha-pregnane-20-one (allopregnanolone) is a potent endogenou

5 gnane-3alpha-ol-20-one (pregnanolone), 5beta-pregnane-3, 20-dione (5beta-dihydroprogesterone), and 5b

6 r etherification of hydroxylated 5alpha/beta-pregnane-3,20-dione or 5beta-cholan-3-one precursors.

7 a-O-disubstituted derivatives of 5alpha/beta-pregnane-3,20-dione, among which the 5beta-H-7alpha-benz

8 the amide derivative (3 alpha,5 beta)-20-oxo-pregnane-3-carboxamide, suggest that the un-ionized form

9 neuroactive steroid, (3 alpha,5 beta)-20-oxo-pregnane-3-carboxylic acid (3 alpha 5 beta PC), with uni

10 dione (5beta-dihydroprogesterone), and 5beta-pregnane-3alpha, 21-diol-20-one (tetrahydrodeoxycorticos

11 19-norandrosterone, androsterone, and 5beta-pregnane-3alpha,17alpha,20alpha-triol (119 ng steroid ab

12 ne, epitestosterone, androsterone, and 5beta-pregnane-3alpha,17alpha,20alpha-triol was fully separate

13 5alpha-Pregnane-3alpha,21-diol-20-one (allotetrahydrodeoxycorti

14 of binding at both sites by GABA and 5alpha-pregnane-3alpha,21-diol-20-one (THDOC), an endogenous an

15 (allotetrahydrodeoxycorticosterone), 5alpha-pregnane-3alpha-ol-11, 20-dione (alphaxalone), and 5alph

16 ha-ol-11, 20-dione (alphaxalone), and 5alpha-pregnane-3alpha-ol-20-one (allopregnanolone) potentiated

17 ne (5alpha-THDOC) potentiates, whereas 5beta-pregnane-3alpha-ol-20-one (pregnanolone) and 5beta-dihyd

18 In contrast, 5beta-pregnane-3alpha-ol-20-one (pregnanolone), 5beta-pregnane

19 of a second potent endogenously synthesized pregnane able to support pregnancy in the absence of pro

20 Derivatives of pregnane and pregnene displayed activities against 5alph

21 s constitutive androstane receptor (CAR) and pregnane and xenobiotic receptor (PXR) in this process.

22 rogesterone, several (mainly 5alpha-reduced) pregnanes are elevated and have long been speculated to

23 Other steroids of the pregnane class induced GSTA2 expression as expected for

24 L-2 and L-10 are delta4-3-one-pregnane derivatives.

25 ith factors binding to the ARE to elicit the pregnane inductive response for GSTA2.

26 d by replacing the androstane nucleus with a pregnane nucleus, provided a ketone at C-20 is present.

27 ct, deletion analysis was used to identify a pregnane responsive region between base pairs -700 and -

28 t the sites of action for the androstane and pregnane series of steroid sulfate blockers of GABA-medi

29 nteractions with GABA(A) receptors, based on pregnane steroids, suggest that the steroid A ring binds

30 Mirasorvone is assigned an 18-oxygenated pregnane structure (structure 9) on the basis of extensi

31 Recently, a series of pregnanes substituted with simple alkyl groups at the 3

32 Together with pregnane X (PXR) and aryl hydrocarbon (AHR) receptors, i

33 oints were related to xenobiotic metabolism (pregnane X and aryl hydrocarbon receptors), hormone-medi

34 The human nuclear pregnane X receptor (hPXR) activates cytochrome P450-3A

35 rapeutic tool.The xenobiotic-activated human pregnane X receptor (hPXR) regulates drug metabolism.

36 The human pregnane X receptor (hPXR) regulates the expression of c

37 Many drugs bind to and activate human pregnane X receptor (hPXR) to upregulate drug-metabolizi

38 ed off-target activities, most notably human pregnane X receptor (hPXR) transactivation, and led to s

39 Human pregnane X receptor (hPXR), an orphan nuclear receptor k

40 bound to RNA polymerase (RNAP) and the human pregnane X receptor (hPXR), representative examples (2b-

41 HNSCC and focused on the role of the nuclear pregnane X receptor (or NR1I2) and epigenetic mechanisms

42 sistance 1 (MDR1 C3435T) P-glycoprotein, and pregnane X receptor (PXR C-25385T, C8055T, and A7635G).

43 mes and drug export pumps, but only one, the pregnane X receptor (PXR in rodents, SXR in humans), reg

44 ehyde-O-(3,4-dichlorobenz yl)oxime (CITCO)], pregnane X receptor (PXR) [rifampicin], and peroxisome p

45 Ketoconazole binds to and antagonizes pregnane X receptor (PXR) activation.

46 Upon treatment with the pregnane X receptor (PXR) activator rifampicin (RIF), hu

47 The pregnane X receptor (PXR) acts as a receptor to induce g

48 sm by which the nuclear xenobiotic receptors pregnane X receptor (PXR) and constitutive active/andros

49 The orphan nuclear receptors pregnane X receptor (PXR) and constitutive androstane re

50 The nuclear pregnane X receptor (PXR) and constitutive androstane re

51 dicates that xenobiotic sensors, such as the pregnane X receptor (PXR) and constitutive androstane re

52 The nuclear receptors pregnane X receptor (PXR) and constitutive androstane re

53 Statins utilize pregnane X receptor (PXR) and serum/glucocorticoid regul

54 , a by-product of intestinal flora, activate pregnane X receptor (PXR) and subsequent CYP3A4 and CYP2

55 The pregnane X receptor (PXR) and the constitutive androstan

56 s constitutive androstane receptor (CAR) and pregnane X receptor (PXR) are involved in the transcript

57 Constitutive androstane receptor (CAR) and pregnane X receptor (PXR) are xenobiotic sensors that en

58 The steroid and xenobiotic-responsive human pregnane X receptor (PXR) binds a broad range of structu

59 The pregnane X receptor (PXR) detects the presence of a wide

60 investigated whether the xenobiotic receptor pregnane X receptor (PXR) has a role in pathogenesis of

61 Ralpha) as well as its heterodimeric partner pregnane X receptor (PXR) in mice.

62 CYP3A4, hepatocyte nuclear factor-4alpha, or pregnane X receptor (PXR) in PHHs.

63 Here we show that the pregnane X receptor (PXR) interacts more strongly with S

64 The pregnane X receptor (PXR) is a key regulator of xenobiot

65 Pregnane X receptor (PXR) is a ligand-dependent transcri

66 The pregnane X receptor (PXR) is a master regulator of xenob

67 The pregnane X receptor (PXR) is a master regulator of xenob

68 Pregnane X receptor (PXR) is a nuclear receptor consider

69 The pregnane X receptor (PXR) is a nuclear receptor signific

70 The human pregnane X receptor (PXR) is a promiscuous nuclear recep

71 Pregnane X receptor (PXR) is a xenobiotic receptor that

72 The nuclear receptor pregnane X receptor (PXR) is activated by a range of xen

73 The pregnane X receptor (PXR) is an important transcriptiona

74 The pregnane X receptor (PXR) is an orphan nuclear receptor

75 Pregnane X receptor (PXR) is known to function as a xeno

76 The nuclear xenobiotic receptor pregnane X receptor (PXR) is promiscuously activated by

77 The pregnane X receptor (PXR) is the molecular target for ca

78 Pregnane X receptor (PXR) mediates xenobiotic and endobi

79 GSTA2 and expression plasmids for either GR, pregnane X receptor (PXR) or a combination of both.

80 The nuclear pregnane X receptor (PXR) plays a central role in regula

81 In mammals the pregnane X receptor (PXR) plays a key role in the regula

82 Pregnane X receptor (PXR) plays an important role in det

83 The pregnane X receptor (PXR) plays an important role in the

84 constitutive androstane receptor (CAR), and pregnane X receptor (PXR) regulate and alter the metabol

85 The human pregnane X receptor (PXR) regulates genes involved in dr

86 Upon drug activation, the nuclear pregnane X receptor (PXR) regulates not only hepatic dru

87 The pregnane X receptor (PXR) regulates the metabolism and e

88 By employing a pregnane X receptor (PXR) reporter gene assay to priorit

89 The human nuclear receptor pregnane X receptor (PXR) responds to a wide variety of

90 man hepatocytes, but does not activate human pregnane X receptor (PXR) significantly in cell-based tr

91 iosgenin increased the expression of several pregnane X receptor (PXR) target genes and the cholereti

92 nduced by the farnesoid X receptor (FXR) and pregnane X receptor (PXR) through the same IR0.

93 The pregnane X receptor (PXR) was isolated as a xenosensor r

94 Pregnane X receptor (PXR) was originally characterized a

95 ells had reduced nuclear localization of the pregnane X receptor (PXR), a key transcriptional regulat

96 Pregnane X receptor (PXR), a member of the NR1I nuclear

97 In contrast, expression levels of the pregnane X receptor (PXR), a nuclear receptor most simil

98 cluding BPA, have been shown to activate the pregnane X receptor (PXR), a nuclear receptor that funct

99 Pregnane X receptor (PXR), a previously known "xenobioti

100 Recent reports suggest that pregnane X receptor (PXR), a xenobiotic nuclear receptor

101 in was transcriptionally up-regulated by the pregnane X receptor (PXR), a xenobiotic-activated nuclea

102 Pregnane X receptor (PXR), acting as a xenobiotic-activa

103 ydrocarbon receptor (AhR), activation of the pregnane X receptor (PXR), activation of the estrogen re

104 The pregnane X receptor (PXR), along with its sister recepto

105 The human pregnane X receptor (PXR), also known as steroid and xen

106 eptors including farnesoid X receptor (FXR), pregnane X receptor (PXR), and constitutive active/andro

107 tream promoter-transcription factor COUP-TF, pregnane X receptor (PXR), and hepatocyte nuclear factor

108 ar receptors, farnesoid X receptor (FXR) and pregnane X receptor (PXR), are important in maintaining

109 cells and hepatoma cells overexpressing the pregnane X receptor (PXR), but not in hepatoma cells in

110 al regulation by nuclear factors such as the pregnane X receptor (PXR), constitutive androstane recep

111 f CYP2B6 and CYP3A4, targets of hCAR and the pregnane X receptor (PXR), in HPH, HepaRG, and PXR-knock

112 e investigated the role of nuclear receptor, pregnane X receptor (PXR), in M. tuberculosis infection

113 s constitutive androstane receptor (CAR) and pregnane X receptor (PXR), respectively.

114 -carbonitrile (PCN), a ligand for the rodent pregnane X receptor (PXR), significantly enhances the ra

115 uman (h) orphan nuclear receptor, termed the pregnane X receptor (PXR), that binds to a response elem

116 a novel orphan nuclear receptor, termed the pregnane X receptor (PXR), that is activated by naturall

117 y increased in mice lacking the SXR ortholog pregnane X receptor (PXR), thereby demonstrating a direc

118 promoter element has been shown to bind the pregnane X receptor (PXR), this receptor does not mediat

119 to the hCAR: PK1195 strongly activated human pregnane X receptor (PXR), whereas it did not alter the

120 mplicated in activating the nuclear receptor pregnane X receptor (PXR), which acts as a xenobiotic se

121 expression is transcriptionally regulated by pregnane X receptor (PXR), which is a ligand-dependent t

122 Here, using a pregnane X receptor (PXR)-humanized mouse model, we foun

123 id, antimineralocorticoid, progestogenic and pregnane X receptor (PXR)-like activities (mug standard-

124 olished in hepatocyte cultures prepared from pregnane X receptor (PXR)-null mice, and cotransfection

125 n CYP3A4-null animals, suggesting that other pregnane X receptor (PXR)-regulated pathways may contrib

126 tagonists have been identified for the human pregnane X receptor (PXR).

127 vated the human nuclear xenobiotic receptor, pregnane X receptor (PXR).

128 multiple mechanisms, including activation of pregnane X receptor (PXR).

129 hift assays showed that CAR-RE binds CAR and pregnane X receptor (PXR).

130 s regulated by nuclear receptors such as the pregnane X receptor (PXR).

131 e constitutive androstane receptor (CAR) and pregnane X receptor (PXR).

132 rier function through the xenobiotic sensor, pregnane X receptor (PXR).

133 ted during confluence in a process involving pregnane X receptor (PXR).

134 n of constitutive androstane receptor and/or pregnane X receptor (PXR).

135 nuclear receptors, including the xenobiotic pregnane X receptor (PXR); (c) the ability to induce hum

136 own that MRP2 expression is regulated by the pregnane X receptor (PXR, NR1I2) and constitutive andros

137 The pregnane X receptor (PXR, NR1I2) is a xenobiotic-sensing

138 Ligand-mediated activation of the pregnane X receptor (PXR, NR1I2) is postulated to affect

139 Pregnane X receptor (PXR, NR1I2), a member of the superf

140 Recently, the pregnane X receptor (PXR, NR1I2), initially characterize

141 that the ligand-activated nuclear receptors pregnane X receptor (PXR; NR1I2) and constitutive andros

142 ers of the nuclear receptor superfamily, the pregnane X receptor (PXR; NR1I2) and constitutive andros

143 ptor (CAR; NR1I3) and to a lesser extent the pregnane X receptor (PXR; NR1I2) are responsible for med

144 itutive androstane receptor (CAR; NR1I3) and pregnane X receptor (PXR; NR1I2), respectively.

145 genes can be targeted for regulation by the pregnane X receptor activator pregnenolone-16alpha-carbo

146 Cotreatment with the prototypical pregnane X receptor activator, rifampicin, significantly

147 sults identify a novel mode of regulation of pregnane x receptor activity and highlight prominent fun

148 protein kinase-mediated repression of human pregnane x receptor activity.

149 ation of the intestinal xenobiotic receptors pregnane X receptor and constitutive androstane receptor

150 ng pathway, which is a critical regulator of pregnane X receptor and hepatocyte nuclear factor 1alpha

151 ic AMP-dependent protein kinase signaling on pregnane x receptor and provide a molecular explanation

152 to determine whether the interaction between pregnane x receptor and these key biochemical pathways i

153 of the protein in vivo indicates that human pregnane x receptor exists as a phosphoprotein and that

154 Pregnane x receptor is a ligand-activated transcription

155 We also report that pregnane X receptor is essential to maintain robust in v

156 The mouse pregnane X receptor is highly similar to the human ortho

157 These findings suggest that treatment with pregnane X receptor ligands may be useful clinically in

158 f CYP3a13 by dexamethasone occurring only in pregnane X receptor null mice.

159 RDelta8 did not repress the nuclear receptor pregnane X receptor or estrogen receptor alpha but did r

160 These data demonstrate an impact of pregnane X receptor polymorphisms on tacrolimus pharmaco

161 We show that the human pregnane x receptor protein can serve as an effective su

162 arbonitrile to activate the nuclear receptor pregnane X receptor restores P-glycoprotein expression a

163 Expression of other pregnane X receptor target enzymes and transporter genes

164 that topotecan and etoposide are ligands of pregnane X receptor that induce CYP3A4 transcription.

165 signaling also modulates the interactions of pregnane x receptor with protein cofactors.

166 tutive androstane receptor) (NR1I3) and PXR (pregnane X receptor) (NR1I2) was generated to study thei

167 xenobiotic-activated nuclear receptors PXR (pregnane X receptor) and CAR (constitutive androstane re

168 role of the nuclear xenobiotic receptor PXR (pregnane X receptor) in this process.

169 The nuclear receptor PXR (pregnane X receptor) is a broad-specificity sensor that

170 The nuclear receptor PXR (pregnane X receptor) protects the body from hepatotoxici

171 biotic receptor) and its rodent homolog PXR (pregnane X receptor) serve as functional bile acid recep

172 loss of the nuclear xenobiotic receptor PXR (pregnane X receptor), a regulator of enterohepatic drug

173 ncoding P-glycoprotein), NR1I2 (encoding the pregnane X receptor), and PPIA (encoding cyclophilin).

174 (CXD2), as well as induction by rifampicin (pregnane X receptor).

175 y, is a potent ligand (K(i) = 27 nM) for the pregnane X receptor, an orphan nuclear receptor that reg

176 the nuclear receptors farsenoid X receptor, pregnane X receptor, and constitutive androstane recepto

177 ative binding sites for retinoid X receptor, pregnane X receptor, and estrogen receptor.

178 receptors constitutive androstane receptor, pregnane X receptor, and peroxisome proliferator-activat

179 including constitutive androstane receptor, pregnane X receptor, and retinoid X receptor (RXR), modu

180 s: farnesoid X receptor, vitamin D receptor, pregnane X receptor, and TGR5.

181 as enhanced in mice lacking the SXR ortholog pregnane X receptor, and treatment of humans with the SX

182 ity is opposite to the sensitizing effect of pregnane X receptor, constitutive androstane receptor, a

183 ilirubinemia can be reduced by activation of pregnane X receptor, constitutive androstane receptor, o

184 ptors, constitutive androstane receptor, and pregnane X receptor, these results suggest that decrease

185 h the ability of these compounds to activate pregnane X receptor-dependent pathways in vivo.

186 ein kinase signaling pathway synergizes with pregnane x receptor-mediated gene activation in mouse he

187 inase signaling has a repressive effect upon pregnane x receptor-mediated gene activation in rat and

188 Both constitutive and pregnane X receptor-mediated inducible activities were m

189 Furthermore, IL-6 attenuated pregnane X receptor-mediated transcription of the CYP3A2

190 The effect of IL-6 on pregnane X receptor-mediated transcription of the rat CY

191 n at 24 hrs, potentially via IL-6 effects on pregnane X receptor-mediated transcription.

192 involve the glucocorticoid receptor and the pregnane X receptor.

193 ling modulates the phosphorylation status of pregnane x receptor.

194 pathways and biological functions, including pregnane X receptor/retinoic acid receptor activation as

195 e acids as CYP3A4 inducers and activators of pregnane X receptor/steroid and xenobiotic receptor (PXR

196 Pregnane X, encoded by the gene NR112, is a nuclear rece

197 as well as agonists of progesterone (PR) and pregnane-X (PXR) receptors did not block the effects of

198 ted with rifampicin in order to identify new pregnane-X receptor (PXR) target genes.

199 Genes encoding CYP3A6, in addition to the pregnane-X-receptor (PXR) and P-glycoprotein (P-gp) were