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 entiating effect of the neurosteroids 5alpha-pregnane-3alpha,21-diol-20-one (THDOC) and progesterone

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

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

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

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

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

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

21 Derivatives of pregnane and pregnene displayed activities against 5alph

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

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

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

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

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

27 creased members of the neuroactive steroidal pregnane molecular family; and that Test diet reduced th

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

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

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

31 One pathway generates pregnane steroids, known in other animals to support rep

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

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

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

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

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

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

38 Activation of human pregnane X receptor (hPXR) has been associated with indu

39 ein receptors to which PFASs bind, the human pregnane X receptor (hPXR) is found to be a host for a v

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

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

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

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

44 A potent agonist of the human pregnane X receptor (hPXR) was designed from two ligands

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

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

47 itutive androstane receptor (hCAR) and human pregnane X receptor (hPXR).

48 atter exhibiting potent agonism on the human pregnane X receptor (hPXR).

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

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

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

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

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

54 er intraperitoneal treatment with the rodent pregnane X receptor (PXR) activator 5-pregnen-3beta-ol-2

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

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

57 Pregnane X receptor (PXR) and AhR-mediated activities we

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

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

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

61 the molecular basis of crosstalk between the pregnane X receptor (PXR) and constitutive androstane re

62 expression of xenobiotic nuclear receptors, pregnane X receptor (PXR) and constitutive androstane re

63 The xenobiotic receptors pregnane X receptor (PXR) and constitutive androstane re

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

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

66 xenobiotic receptor [SXR; also known as the pregnane X receptor (PXR) and formally known as NR1I2] i

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

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

69 anscription-factor interactions, namely, the pregnane X receptor (PXR) and the aryl hydrocarbon recep

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

71 ion, is shown here to directly bind to human pregnane X receptor (PXR) and thereby act as a partial a

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

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

74 uided optimization with respect to decreased pregnane X receptor (PXR) binding was started.

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

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

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

78 Pregnane X receptor (PXR) has been reported to regulate

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

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

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

82 The pregnane X receptor (PXR) is a key regulator of drug met

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

84 The pregnane X receptor (PXR) is a ligand-activated regulato

85 Pregnane X receptor (PXR) is a ligand-activated transcri

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

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

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

89 Pregnane X receptor (PXR) is a master xenobiotic-sensing

90 The pregnane X receptor (PXR) is a nuclear receptor (NR), in

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

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

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

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

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

96 The pregnane X receptor (PXR) is an important regulator of h

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

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

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

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

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

102 mponent, furanodienone (FDN), is a selective pregnane X receptor (PXR) ligand with agonistic transcri

103 Pregnane X receptor (PXR) mediates xenobiotic and endobi

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

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

106 The pregnane X receptor (PXR) plays a fundamental role in re

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

108 form with the retinoid X receptor (RXR), the pregnane X receptor (PXR) plays an essential role in con

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

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

111 Pregnane X receptor (PXR) plays roles in detoxification

112 me) have limited selectivity, activating the pregnane X receptor (PXR) receptor, a related receptor o

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

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

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

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

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

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

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

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

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

122 The aryl hydrocarbon receptor (AhR) and pregnane X receptor (PXR) transcription factors showed t

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

124 ARgamma activity, and specific activation of pregnane X receptor (PXR) was observed together with Apo

125 Pregnane X receptor (PXR) was originally characterized a

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

127 The pregnane X receptor (PXR), a ligand-activated nuclear re

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

129 e sought to interrogate the influence of the pregnane X receptor (PXR), a modulator of xenobiotic and

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

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

132 aphy to characterize a structural feature of pregnane X receptor (PXR), a nuclear receptor that is ac

133 and the BET-inactive (-)-JQ1 are agonists of pregnane X receptor (PXR), a nuclear receptor that trans

134 (SJW), from traditional herbs, activates the pregnane X receptor (PXR), a potential drug target for t

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

136 been reported regarding PB regulation of the pregnane X receptor (PXR), a sister receptor of CAR, and

137 fampicin and efavirenz are activators of the pregnane X receptor (PXR), a transcription factor with s

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

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

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

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

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

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

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

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

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

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

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

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

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

151 We found that chemicals activating the pregnane X receptor (PXR), peroxisome proliferator recep

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

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

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

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

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

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

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

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

160 Xenosensing pregnane X receptor (PXR), which also participates in th

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

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

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

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

165 Experiments performed using pregnane X receptor (PXR)-null mouse hepatocytes reveale

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

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

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

169 ession by activation of the nuclear receptor pregnane X receptor (PXR).

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

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

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

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

174 potently activate the human nuclear receptor pregnane X receptor (PXR).

175 mouse liver in response to the activation of pregnane X receptor (PXR).

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

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

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

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

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

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

182 e have previously shown that the xenosensing pregnane x receptor (pxr, nr1i2) is lost in many teleost

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

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

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

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

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

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

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

190 ebulette (Nebl) to be efficiently induced by pregnane X receptor activating compounds.

191 er intraperitoneal treatment with the rodent pregnane X receptor activator 5-pregnen-3beta-ol-20-one-

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

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

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

195 ibited progesterone, estrogen, androgen, and pregnane X receptor activity, albeit generally with redu

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

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

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

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

200 ctivated transcription factors including the pregnane X receptor and the aryl hydrocarbon receptor.

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

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

203 Protein structure information on the pregnane X receptor helped in overcoming a persistent cy

204 xons with the Nebl gene is a novel target of pregnane X receptor in mouse liver.

205 Pregnane x receptor is a ligand-activated transcription

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

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

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

209 by the constitutive androstane receptor and pregnane X receptor nuclear receptors.

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

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

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

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

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

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

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

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

218 tion in CD4(+) T cells(3) and agonism of the pregnane X receptor(4).

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

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

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

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

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

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

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

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

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

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

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

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

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

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

233 ers, expression of nuclear receptors CAR and pregnane X receptor, and structure of the ALDH1A7 promot

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

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

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

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

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

239 Elevated bile acids activated pregnane X receptor, which was sufficient to recapitulat

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

241 her supports this finding but shows that the pregnane X receptor-ligand hyperforin is not the driving

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

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

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

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

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

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

248 involve the glucocorticoid receptor and the pregnane X receptor.

249 ling modulates the phosphorylation status of pregnane x receptor.

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

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

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

253 ty, reducing active efflux, and addressing a pregnane X-receptor liability.

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

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

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

257 This perspective discusses the role of pregnane xenobiotic receptor (PXR) in drug discovery and