ライフサイエンスコーパス: PXR

1 PXR ablation inhibited high-fat diet (HFD)-induced obesi

2 PXR activation by PCN in high-fat diet fed mice also inc

3 PXR also contributes to the dysregulation of these proce

4 PXR antagonists 20 and 24 (IC50 = 14 muM), in addition t

5 PXR associates with multiple corepressors that attenuate

6 PXR expression was increased, and PXR protein accumulate

7 PXR indirectly activated the IGFBP1 gene by repressing t

8 PXR is a key regulator of pregnancy induced glucuronidat

9 PXR ligand-mediated inhibition of platelet function was

10 PXR plays a vital role in the drug metabolism pathway, a

11 PXR was found to modulate RTV hepatotoxicity through CYP

12 PXR-deficient (Nr1i2(-/-)) mice showed a distinctly "lea

13 ld) and its target, Cyp2b10 (220-fold), in a PXR-dependent manner.

14 Interestingly, a PXR variant with a naturally occurring deletion of a con

15 A luciferase reporter assay on a PXR-transfected HepG2 cell line identified compounds 19-

16 tribromoethanol (Avertin) in vivo, abrogates PXR-mediated resistance to 7-ethyl-10-hydroxycamptotheci

17 determine whether they bind to and activate PXR.

18 mechanism by which these chemicals activate PXR remains unknown.

19 molecule CAR inhibitors that do not activate PXR.

20 Amprenavir efficiently activated PXR and induced PXR target gene expression in vitro and

21 that ketoconazole binds to ligand-activated PXR and antagonizes receptor control of gene expression.

22 Statin-activated PXR scaffolds the protein phosphatase 2C (PP2C) and SGK2

23 sm by which BPA interacts with and activates PXR and examined selected BPA analogues to determine whe

24 Non-phosphorylated SGK2 co-activates PXR-mediated trans-activation of promoters of gluconeoge

25 vity relationship studies of the most active PXR antagonist from the series (compound 20, IC50 = 11 m

26 e variable with similarities of 60%-100% and PXR, CAR, DAX1 and SHP were least conserved among specie

27 metabolism and transport (CYP3A5, ABCB1, and PXR) were analyzed in kidney transplant recipients (1995

28 Surface waters with AhR and PXR effects were associated with low intensity, develope

29 icals did not completely account for AhR and PXR responses.

30 ned to study the interaction between BPA and PXR.

31 ion of CYP1A, CYP2B6 and CYP3A4 (for CAR and PXR), and CYP2C8 (for PXR) gene expression.

32 ement of beta-catenin in the AhR-, CAR-, and PXR-mediated induction of CYP1A, CYP2B6 and CYP3A4 (for

33 nfluent resulted in a decrease in CYP3A4 and PXR expression back to levels observed in subconfluent c

34 dying the regulation/induction of CYP3A4 and PXR is critical in toxicology and drug-drug interaction

35 significantly increases the basal CYP3A4 and PXR levels in 24 hours.

36 ating control cells increased the CYP3A4 and PXR protein levels.

37 ey express negligible amounts of CYP450s and PXR.

38 egnane X receptor (PXR), in HPH, HepaRG, and PXR-knockout HepaRG cells.

39 network identified HNF4alpha, HNF1alpha, and PXR.

40 PXR expression was increased, and PXR protein accumulated in the nuclei during confluent g

41 onicasterol E represents a FXR modulator and PXR agonist that might hold utility in treatment of live

42 ication between the intestinal symbionts and PXR regulates mucosal integrity through a pathway that i

43 blish PXR as a novel therapeutic target, and PXR antagonists may be used for the prevention and treat

44 ing male PXR-humanized (hPXR) transgenic and PXR-knock-out (PXR-KO) mice in comparison to wild-type (

45 t for "xenobiotic metabolism signaling" and "PXR/RXR activation" pathways.

46 colon cancer cells in vitro, and attenuates PXR-mediated acetaminophen hepatotoxicity in vivo.

47 In fact, currently available PXR ligands are not highly selective and can exhibit tox

48 Following intrarectal exposure to TcdA/B, PXR-deficient mice (Nr1i2(-/-) ) exhibited reduced survi

49 scovery of novel bazedoxifene-scaffold-based PXR antagonists inspired by the marine sulfated steroids

50 tabolic liabilities including bioactivation, PXR activation, as well as CYP3A4 induction and inhibiti

51 Both PXR activation and deficiency promote hepatic triglyceri

52 reas an anti-IGFBP1 antibody attenuated both PXR-induced morphological changes and migration in ShP51

53 were resistant to HFD-induced obesity, both PXR-KO and hPXR mice exhibited impaired induction of glu

54 We further show that both PXR and RXRalpha bind to the transcriptional coregulator

55 r pathophysiological conditions regulated by PXR and AhR.

56 CAR, PXR and ESR1 were found to be the most important trans-r

57 that involves the energy status of the cell, PXR regulation, and drug sensitivity.

58 rfering RNA knockdown of HNF4alpha connected PXR-mediated gene regulation with the PXR-induced cellul

59 Decreased PXR binding to the CYP3A4 proximal promoter was found in

60 Activation of AMPK was shown to downregulate PXR activity and, consistent with that, potentiate the r

61 garcinoic acid as a selective and efficient PXR agonist.

62 Our results may help to establish PXR as a novel therapeutic target, and PXR antagonists m

63 wildtype (WT) and Pxr-null mice, we examined PXR-mediated regulation of chronic EtOH-induced hepatic

64 epG2-derived ShP51 cells that stably express PXR showed epithelial-mesenchymal transition (EMT)-like

65 Interestingly, control-fed PXR-KO mice exhibited hepatomegaly, hyperinsulinemia, an

66 An FGF21-PXR signaling pathway may be involved in decreased hepat

67 One fluorescent PXR probe is currently commercially available; however,

68 nd CYP3A4 (for CAR and PXR), and CYP2C8 (for PXR) gene expression.

69 hydroxyl groups as hydrogen-bond donors for PXR antagonistic activity.

70 ), in the context of indole, is a ligand for PXR in vivo, and IPA downregulated enterocyte TNF-alpha

71 We now report a novel role for PXR as a critical negative regulator of innate immunity

72 In summary, we discovered an apical role for PXR in regulating innate immunity.

73 ha-IGFBP1 pathway is an essential signal for PXR-induced morphological changes and migration.

74 which BPA interacts with and activates human PXR.

75 FL in its function as a high-affinity human PXR ligand.

76 4, two shared target genes of hCAR and human PXR (hPXR).

77 describe a BODIPY FL-vinblastine-based human PXR time-resolved fluorescence resonance energy transfer

78 its analogues are potent agonists for human PXR (hPXR) but do not affect mouse PXR activity.

79 IPY FL), as a high-affinity ligand for human PXR with a Kd value of 673 nM.

80 uish the function of hCAR from that of human PXR (hPXR).

81 ng the expression and functionality of human PXR (hPXR).

82 rk demonstrated the essential roles of human PXR and CYP3A4 in RTV hepatotoxicity, which can be appli

83 between the ligand-binding domains of human PXR and RXRalpha.

84 ides a model for exploring the role of human PXR in the metabolic syndrome.

85 s used to successfully test a panel of human PXR ligands.

86 nus carpio) primary hepatocytes to the human PXR agonist rifampicin (RIF) on expression of target gen

87 icularly mycolic acids, crosstalk with human PXR (hPXR) by interacting with its promiscuous ligand bi

88 uate thrombus formation in vivo in humanised PXR transgenic mice.

89 This study identifies PXR as both a positive and negative regulator of the UGT

90 rmed a mass spectrometric screen to identify PXR-associated proteins.

91 and to avoid the reported species barrier in PXR function, we adopted an in vivo mouse model expressi

92 tagonist binding on the surface or buried in PXR indicates novel aspects to the mechanism of receptor

93 esterol levels in wild-type mice, but not in PXR-deficient mice.

94 ic and pharmacokinetic properties, including PXR activation, CYP2C9 inhibition, and CYP3A4 TDI, sever

95 BPA and its analogues can also induce PXR target gene expression in human LS180 cells.

96 enavir efficiently activated PXR and induced PXR target gene expression in vitro and in vivo.

97 e of OATP2B1 enhanced the hyperforin-induced PXR activation in cell-based luciferase assays.

98 Finally, vemurafenib strongly induced PXR activity in vitro, but only weakly induced PXR in vi

99 R activity in vitro, but only weakly induced PXR in vivo.

100 These results provide new insights into PXR-mediated cellular responses toward xenobiotics inclu

101 compared our screen results identifying key PXR residues to those predicted by computational methods

102 substituents on the ether linker led to less PXR binding while maintaining the P2X4 inhibitory potenc

103 Cell-based reporter assays, in silico ligand-PXR docking studies, and site-directed mutagenesis were

104 losed, it is not optimal for studying ligand-PXR interactions.

105 HFD)-induced obesity was examined using male PXR-humanized (hPXR) transgenic and PXR-knock-out (PXR-K

106 Amprenavir-mediated PXR activation stimulated the expression of several key

107 structural information was used to modulate PXR affinity for a related CCR1 antagonist compound that

108 MP-activated protein kinase (AMPK) modulates PXR transcriptional activity and that pharmacologically

109 ntagonist, SPA70; 3) does not activate mouse PXR; 4) depends on tryptophan-299 to activate hPXR; 5) r

110 for human PXR (hPXR) but do not affect mouse PXR activity.

111 eceptor coactivator-1 and hPXR but not mouse PXR.

112 Altogether, although the mouse PXR promotes HFD-induced obesity, the hPXR mouse carries

113 ligand specificities between human and mouse PXRs, the role of PXR in high fat diet (HFD)-induced obe

114 her xenobiotic or hormonal receptors, namely PXR, AHR, and vitamin D receptor, which regulate major x

115 lead compound toward the development of new PXR-regulating modulators.

116 ne such inhibitor, CINPA1 (CAR inhibitor not PXR activator 1), capable of reducing CAR-mediated trans

117 Of note, PXR deficiency suppressed these changes and steatosis.

118 ation and downregulation of lipin-1, a novel PXR target gene.

119 lpha but not 10 other NRs in vivo, while NRs PXR, FXRalpha, Rev-Erbalpha appear to bind adjacent to H

120 tor of CYP3A4 Furthermore, decreased nuclear PXR was observed in mouse liver and Huh7 cells after FGF

121 Activation of PXR by BPA may explain some of the adverse effects of BP

122 Here we report that the activation of PXR by pregnenolone 16alpha-carbonitrile (PCN) in AKR/J

123 Activation of PXR, but not of the closely related constitutive androst

124 CAR inverse-agonists are also activators of PXR, rendering them mechanistically counterproductive in

125 inoic acid is a selective natural agonist of PXR and a promising lead compound toward the development

126 This review highlights areas of PXR regulation that require further clarification and su

127 The metabolic benefit of PXR ablation was opposite to the reported prodiabetic ef

128 Mechanistically, the metabolic benefits of PXR ablation were associated with the inhibition of c-Ju

129 , we showed that p53 inhibits the binding of PXR to the CYP3A4 promoter.

130 The ob/ob mice deficient of PXR showed increased oxygen consumption and energy expen

131 of CYP3A4, and siRNA-mediated knock-down of PXR in confluent cells resulted in decreased CYP3A4 expr

132 4 muM), in addition to the downregulation of PXR expression, exhibited inhibition of PXR-induced CYP3

133 ies acute, non-genomic regulatory effects of PXR ligands on platelet function and thrombus formation.

134 The effects of PXR ligands were observed in a species-specific manner,

135 Evolution of PXR and CAR exhibited unexpected multiple patterns and t

136 pathway, and a comprehensive examination of PXR-associated proteins will provide greater insight int

137 tiating hESCs, and stable over-expression of PXR in hepatic-induced hESCs failed to enhance expressio

138 The expression of PXR in human platelets was confirmed using immunoprecipi

139 erous NRs, we investigated the expression of PXR in platelets along with the ability of its ligands t

140 -hybrid screen that examined mutant forms of PXR.

141 cal for studying the overlapping function of PXR and CAR.

142 ese results verify the important function of PXR in lipid and energy metabolism and suggest that PXR

143 In the past several years, the function of PXR in the regulation of xenobiotic metabolism has been

144 erstanding of the nonxenobiotic functions of PXR that can be explored for relevant therapeutic applic

145 ts uncover SLC13A5 as a novel target gene of PXR and may contribute to drug-induced steatosis and met

146 ous cancer cells indicates the importance of PXR as a drug target for countering multidrug resistance

147 lls is caused by the endogenous induction of PXR as a result of cell-cell contact inhibited prolifera

148 n of PXR expression, exhibited inhibition of PXR-induced CYP3A4 expression, which illustrates their p

149 al hUGT1 hepatocytes through interruption of PXR by small interfering RNA.

150 However, the molecular mechanism of PXR-mediated activation of ethanol (EtOH)-induced steato

151 Modulation of PXR transactivation has revealed the selective and orall

152 The overexpression of PXR in various cancer cells indicates the importance of

153 residues within the ligand-binding pocket of PXR that constitute points of interaction with amprenavi

154 emerging anti-atherosclerotic properties of PXR ligands, these anti-thrombotic effects may provide a

155 dogenous, non-ligand-dependent regulation of PXR and CYP3A4, possibly of physiologic and pharmacologi

156 f BPA and its analogues on the regulation of PXR target genes in human LS180 cells.

157 site that are associated with regulation of PXR-mediated SLC13A5 induction.

158 f the cell cycle and a negative regulator of PXR, was more highly expressed in proliferating control

159 as been extensively studied, and the role of PXR as a xenobiotic sensor has been well established.

160 es between human and mouse PXRs, the role of PXR in high fat diet (HFD)-induced obesity was examined

161 disease and demonstrate a potential role of PXR in mediating the adverse effects of HIV PIs in human

162 e uncovered an unexpected endobiotic role of PXR in obesity and type 2 diabetes.

163 These recent discoveries of the role of PXR in the physiologic and pathophysiologic conditions o

164 discovered previously unidentified roles of PXR in inflammatory response, cell proliferation, and ce

165 define the antagonist binding surface(s) of PXR, we developed a novel assay to identify key amino ac

166 Yeast high throughput screens of PXR mutants define a unique region for ketoconazole bind

167 The unique structure of PXR allows the binding of many drugs and drug leads to i

168 Three different co-crystal structures of PXR LBD with Adnectin-1 and CCR1 (CC chemokine receptor-

169 The structures of PXR with Adnectin-1 reveal specificity of Adnectin-1 in

170 ization chaperones to generate structures of PXR with compounds of interest.

171 f antagonist binding sites on the surface of PXR and suggest new avenues to regulate this receptor fo

172 Gln-272, and Phe-264 on the AF-2 surface of PXR.

173 A5 gene is a novel transcriptional target of PXR, and altered expression of SLC13A5 affects lipid acc

174 her, these data advance our understanding of PXR, the master regulator of drug metabolism gene expres

175 g and hepatocyte death were not dependent on PXR, which is a nuclear receptor transcription factor th

176 assay to identify key amino acid residues on PXR based on a yeast two-hybrid screen that examined mut

177 manized (hPXR) transgenic and PXR-knock-out (PXR-KO) mice in comparison to wild-type (WT) mice.

178 synthetic strategy, and rifaximin, a potent PXR agonist, demonstrated that conicasterol E is an FXR

179 contrast with mammals, where CTZ is a potent PXR-agonist.

180 mprenavir, a widely used HIV PI, as a potent PXR-selective agonist.

181 Collectively our data indicate potential PXR involvement in regulating selected genes involved in

182 line identified compounds 19-24 as promising PXR antagonists.

183 Compared with ketoconazole, a prototypical PXR antagonist, FLB-12 is significantly less toxic to he

184 The prototypical PXR activator rifampicin markedly induced the mRNA and p

185 ed the cloning of the human nuclear receptor PXR and demonstrated that it mediates CYP3A induction.

186 450 enzyme regulated by the nuclear receptor PXR, is involved in most of the drug metabolizing pathwa

187 The human nuclear xenobiotic receptor PXR recognizes a range of potentially harmful drugs and

188 benz yl)oxime (CITCO)], pregnane X receptor (PXR) [rifampicin], and peroxisome proliferator-activated

189 inds to and antagonizes pregnane X receptor (PXR) activation.

190 eatment with the rodent pregnane X receptor (PXR) activator 5-pregnen-3beta-ol-20-one-16alpha-carboni

191 Upon treatment with the pregnane X receptor (PXR) activator rifampicin (RIF), human hepatocellular ca

192 Pregnane X receptor (PXR) and AhR-mediated activities were the most commonly

193 he xenobiotic receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are acti

194 ic sensors, such as the pregnane X receptor (PXR) and constitutive androstane receptor (CAR), may und

195 [SXR; also known as the pregnane X receptor (PXR) and formally known as NR1I2] is a nuclear hormone r

196 Statins utilize pregnane X receptor (PXR) and serum/glucocorticoid regulated kinase 2 (SGK2)

197 estinal flora, activate pregnane X receptor (PXR) and subsequent CYP3A4 and CYP2C9 expression in hPSC

198 teractions, namely, the pregnane X receptor (PXR) and the aryl hydrocarbon receptor (AhR), and itsint

199 tane receptor (CAR) and pregnane X receptor (PXR) are xenobiotic sensors that enhance the detoxificat

200 th respect to decreased pregnane X receptor (PXR) binding was started.

201 clear factor-4alpha, or pregnane X receptor (PXR) in PHHs.

202 The pregnane X receptor (PXR) is a master regulator of xenobiotic metabolism, and

203 Pregnane X receptor (PXR) is a master xenobiotic-sensing transcription factor

204 The pregnane X receptor (PXR) is a nuclear receptor (NR), involved in the detoxif

205 Pregnane X receptor (PXR) is a nuclear receptor considered to be a master xen

206 The human pregnane X receptor (PXR) is a promiscuous nuclear receptor that functions as

207 Pregnane X receptor (PXR) is a xenobiotic receptor that regulates the detoxif

208 Pregnane X receptor (PXR) is known to function as a xenobiotic sensor to regu

209 The nuclear pregnane X receptor (PXR) plays a central role in regulating xenobiotic metab

210 In mammals the pregnane X receptor (PXR) plays a key role in the regulation of a suite of ge

211 The human pregnane X receptor (PXR) regulates genes involved in drug metabolism and dis

212 The pregnane X receptor (PXR) regulates the metabolism and excretion of xenobioti

213 By employing a pregnane X receptor (PXR) reporter gene assay to prioritize compounds for fur

214 rbon receptor (AhR) and pregnane X receptor (PXR) transcription factors showed the greatest upregulat

215 specific activation of pregnane X receptor (PXR) was observed together with ApoE and multidrug resis

216 ear localization of the pregnane X receptor (PXR), a key transcriptional regulator of CYP3A4 Furtherm

217 Pregnane X receptor (PXR), a member of the NR1I nuclear receptor family, acts

218 te the influence of the pregnane X receptor (PXR), a modulator of xenobiotic and detoxification respo

219 xpression levels of the pregnane X receptor (PXR), a nuclear receptor most similar to CAR in primary

220 n shown to activate the pregnane X receptor (PXR), a nuclear receptor that functions as a master regu

221 ng PB regulation of the pregnane X receptor (PXR), a sister receptor of CAR, and the underlying mecha

222 z are activators of the pregnane X receptor (PXR), a transcription factor with significant inter-spec

223 nt reports suggest that pregnane X receptor (PXR), a xenobiotic nuclear receptor important for defens

224 AhR), activation of the pregnane X receptor (PXR), activation of the estrogen receptor (ER), adaptive

225 The pregnane X receptor (PXR), along with its sister receptor constitutive andros

226 ells overexpressing the pregnane X receptor (PXR), but not in hepatoma cells in which PXR was knocked

227 targets of hCAR and the pregnane X receptor (PXR), in HPH, HepaRG, and PXR-knockout HepaRG cells.

228 le of nuclear receptor, pregnane X receptor (PXR), in M. tuberculosis infection in human monocyte-der

229 ng the nuclear receptor pregnane X receptor (PXR), which acts as a xenobiotic sensor to regulate xeno

230 Here, using a pregnane X receptor (PXR)-humanized mouse model, we found that co-treatment w

231 coid, progestogenic and pregnane X receptor (PXR)-like activities (mug standard-EQ/g of sorbent range

232 riments performed using pregnane X receptor (PXR)-null mouse hepatocytes revealed that EFV-mediated X

233 , suggesting that other pregnane X receptor (PXR)-regulated pathways may contribute more significantl

234 the xenobiotic sensor, pregnane X receptor (PXR).

235 in a process involving pregnane X receptor (PXR).

236 of the nuclear receptor pregnane X receptor (PXR).

237 The pregnane X receptor (PXR, NR1I2) is a xenobiotic-sensing nuclear receptor tha

238 Pregnane X receptor (PXR, NR1I2), a member of the superfamily of nuclear rece

239 Recently, the pregnane X receptor (PXR, NR1I2), initially characterized as a xenobiotic sen

240 een shown to act through multiple receptors (PXR, VDR, TGR5 and S1PR2), as well as to have receptor-i

241 e that wild-type p53 can negatively regulate PXR by physically associating with it.

242 quired but not sufficient for p53 to repress PXR activity.

243 rties of this natural molecule as a specific PXR agonist were demonstrated by the screening on a pane

244 conazole genetically interacts with specific PXR surface residues.

245 This gluconeogenic statin-PXR-SGK2 signal is not present in mice, in which statin

246 Here, the novel statin/PXR/SGK2-mediated signaling pathway has now been charact

247 mal cLogD values and the discovery of subtle PXR SAR that was not lipophilicity dependent.

248 hich illustrates their potential to suppress PXR-regulated phase-I drug metabolism.

249 These results support a major role for SXR/PXR in protection against xenobiotic-induced oxidative s

250 s, in particular the glucocorticoids, target PXR as a positive regulator of human glucuronidation.

251 In this study, we demonstrate that PXR augments M. tuberculosis survival inside the host ma

252 These data demonstrated that PXR regulated pathogen-induced inflammation and host def

253 We determined that PXR is expressed in liver, acts through a DNA response e

254 These structures establish that PXR and RXRalpha form a heterotetramer unprecedented in

255 These findings establish that PXR signaling contributes to ALD development and suggest

256 It is now clear, however, that PXR plays many other roles in addition to its xenobiotic

257 Recent studies indicate that PXR may also play an important role in the regulation of

258 We observed that PXR activity was induced under high-glucose conditions.

259 unoprecipitation (ChIP) assays revealed that PXR activation by RIF disrupted enhancer-promoter commun

260 l-based reporter and ChIP assays showed that PXR targeted the distal enhancer of the HNF4alpha P1 pro

261 tributes to ALD development and suggest that PXR antagonists may provide a new approach for ALD thera

262 lipid and energy metabolism and suggest that PXR represents a novel therapeutic target for prevention

263 The PXR ligand rifampicin further increased the expression o

264 ntial of targeting the PXR, we activated the PXR with pregnenolone 16alpha-carbonitrile (PCN) in wild

265 ression of all target genes measured and the PXR antagonist ketoconazole (KET) inhibited responses of

266 MP may be explained, at least partly, by the PXR-dependent transcriptional inhibition of ATX expressi

267 ss than 0.2% of the biological effect in the PXR activation, adaptive stress response, and fish embry

268 horylation-deficient mutation (S350A) in the PXR protein significantly induced the CYP3A4 transcripti

269 FLB-12 significantly inhibits the PXR-activated loss of righting reflex to 2,2,2-tribromoe

270 In an independent model, introducing the PXR(-/-) allele into the ob/ob background also improved

271 nding affinity, and the determination of the PXR-garcinoic acid complex crystal structure.

272 th higher affinity when they are part of the PXR/RXRalpha heterotetramer complex than they do when ea

273 n type III domain ((10)Fn3), that target the PXR ligand binding domain (LBD) interactions with the st

274 s the therapeutic potential of targeting the PXR, we activated the PXR with pregnenolone 16alpha-carb

275 Taken together, these data suggest that the PXR plays a role in the host's response to TcdA/B and ma

276 s cell system, we demonstrated here that the PXR-HNF4alpha-IGFBP1 pathway is an essential signal for

277 d not interact with p53, indicating that the PXR-p53 interaction is specific.

278 nction" mutants that were "resistant" to the PXR antagonist effects of ketoconazole.

279 rized the molecular mechanism underlying the PXR-mediated repression of the HNF4alpha gene.

280 nected PXR-mediated gene regulation with the PXR-induced cellular responses, showing that the knockdo

281 t that modulation of bioavailability through PXR-mediated regulation of drug transporters (e.g., by o

282 toxin protoporphyrin IX in the liver through PXR-mediated alteration of the heme biosynthesis pathway

283 Thus, PXR and p53 appear to play important yet opposing roles

284 Thus, PXR represses human SULT1E1, possibly attenuating the in

285 Thus, PXR serves to repress UGT1A1 gene expression during deve

286 ues that are involved in binding of SRC-1 to PXR.

287 l to evaluate whether lead compounds bind to PXR.

288 g to evaluate whether lead compounds bind to PXR.

289 K activation exhibits an inverse relation to PXR activity.

290 azole and a 10-fold induction in response to PXR agonist rifampicin.

291 Using PXR-humanized mouse models, we recapitulated the RTV hep

292 Employing reverse genetics, where PXR has been genetically deleted, hUGT1/Pxr(-/-) mice sh

293 nsitivity to chemotherapeutic drugs, whereas PXR contributes to chemoresistance in many cancer cells.

294 WT mice showed greater weight gain, whereas PXR-KO mice gained less weight due to their resistance t

295 or (PXR), but not in hepatoma cells in which PXR was knocked down.

296 or suppressor protein p53 can associate with PXR and downregulate its activity.

297 icasterol E is an FXR modulator endowed with PXR agonistic activity.

298 e p53 by competing with its interaction with PXR, suggesting that protein-protein interaction is requ

299 f-function p53 mutant (R175H) interacts with PXR but does not repress its activity.

300 Treatment with PXR ligands was found to inhibit platelet functions stim

301 Together with pregnane X (PXR) and aryl hydrocarbon (AHR) receptors, it is referre