NR1I2

Summary

Gene Symbol: NR1I2
Description: nuclear receptor subfamily 1 group I member 2
Alias: BXR, ONR1, PAR, PAR1, PAR2, PARq, PRR, PXR, SAR, SXR, nuclear receptor subfamily 1 group I member 2, orphan nuclear receptor PAR1, orphan nuclear receptor PXR, pregnane X nuclear receptor variant 2, pregnane X receptor, steroid and xenobiotic receptor
Species: human
Products:     NR1I2

Top Publications

  1. Kliewer S, Moore J, Wade L, Staudinger J, Watson M, Jones S, et al. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell. 1998;92:73-82 pubmed
    ..We describe a novel orphan nuclear receptor, termed the pregnane X receptor (PXR), that is activated by naturally occurring steroids such as pregnenolone and progesterone, and ..
  2. Jiang H, Chen K, He J, Pan F, Li J, Chen J, et al. Association of pregnane X receptor with multidrug resistance-related protein 3 and its role in human colon cancer chemoresistance. J Gastrointest Surg. 2009;13:1831-8 pubmed publisher
    Pregnane xenobiotic receptor (PXR), a ligand-activated transcription factor, regulates the drug metabolism and transport. Its activation can reduce the efficacy of antineoplastic agents...
  3. Fanta S, Niemi M, Jönsson S, Karlsson M, Holmberg C, Neuvonen P, et al. Pharmacogenetics of cyclosporine in children suggests an age-dependent influence of ABCB1 polymorphisms. Pharmacogenet Genomics. 2008;18:77-90 pubmed publisher
    To evaluate whether variations in the ABCB1, ABCC2, SLCO1B1, CYP3A4, CYP3A5, or NR1I2 genes are associated with the pharmacokinetics of cyclosporine in pediatric renal transplant candidates, and whether the effects of these variants are ..
  4. Ouyang N, Ke S, Eagleton N, Xie Y, Chen G, Laffins B, et al. Pregnane X receptor suppresses proliferation and tumourigenicity of colon cancer cells. Br J Cancer. 2010;102:1753-61 pubmed publisher
    b>Pregnane X receptor (PXR) is a nuclear receptor that regulates the metabolism and disposition of various xenobiotics and endobioitics. We investigated a novel PXR function in regulating colon tumourigenesis in this study...
  5. Dring M, Goulding C, Trimble V, Keegan D, Ryan A, Brophy K, et al. The pregnane X receptor locus is associated with susceptibility to inflammatory bowel disease. Gastroenterology. 2006;130:341-8; quiz 592 pubmed
    The pregnane X receptor (PXR) regulates an array of genes involved in the response to xenobiotics...
  6. Wang H, Venkatesh M, Li H, Goetz R, Mukherjee S, Biswas A, et al. Pregnane X receptor activation induces FGF19-dependent tumor aggressiveness in humans and mice. J Clin Invest. 2011;121:3220-32 pubmed publisher
    The nuclear receptor pregnane X receptor (PXR) is activated by a range of xenochemicals, including chemotherapeutic drugs, and has been suggested to play a role in the development of tumor cell resistance to anticancer drugs...
  7. Lehmann J, McKee D, Watson M, Willson T, Moore J, Kliewer S. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J Clin Invest. 1998;102:1016-23 pubmed
    ..We report the identification of a human (h) orphan nuclear receptor, termed the pregnane X receptor (PXR), that binds to a response element in the CYP3A4 promoter and is activated by a range of drugs known ..
  8. Gupta D, Venkatesh M, Wang H, Kim S, Sinz M, Goldberg G, et al. Expanding the roles for pregnane X receptor in cancer: proliferation and drug resistance in ovarian cancer. Clin Cancer Res. 2008;14:5332-40 pubmed publisher
    We examined the presence of the pregnane X receptor (PXR) and its effects on ovarian cancer cells after activation by its cognate ligand...
  9. Takagi S, Nakajima M, Mohri T, Yokoi T. Post-transcriptional regulation of human pregnane X receptor by micro-RNA affects the expression of cytochrome P450 3A4. J Biol Chem. 2008;283:9674-80 pubmed publisher
    b>Pregnane X receptor (PXR) is a major transcription factor regulating the inducible expression of a variety of transporters and drug-metabolizing enzymes, including CYP3A4 (cytochrome P450 3A4)...

More Information

Publications78

  1. Kojima K, Nagata K, Matsubara T, Yamazoe Y. Broad but distinct role of pregnane x receptor on the expression of individual cytochrome p450s in human hepatocytes. Drug Metab Pharmacokinet. 2007;22:276-86 pubmed
    In the present study, we have utilized a target selective human pregnane X receptor-siRNA (hPXR-siRNA)-adenovirus expression system to examine the contribution of hPXR on the gene regulation of drug-metabolizing P450s in human ..
  2. Zhou C, Tabb M, Nelson E, Grün F, Verma S, Sadatrafiei A, et al. Mutual repression between steroid and xenobiotic receptor and NF-kappaB signaling pathways links xenobiotic metabolism and inflammation. J Clin Invest. 2006;116:2280-2289 pubmed
    ..Here we show that activation of the nuclear steroid and xenobiotic receptor (SXR) by commonly used drugs in humans inhibits the activity of NF-kappaB, a key regulator of ..
  3. Ferguson S, Chen Y, LeCluyse E, Negishi M, Goldstein J. Human CYP2C8 is transcriptionally regulated by the nuclear receptors constitutive androstane receptor, pregnane X receptor, glucocorticoid receptor, and hepatic nuclear factor 4alpha. Mol Pharmacol. 2005;68:747-57 pubmed
    ..5'-flanking region of CYP2C8 and investigated its transcriptional regulation by nuclear factors such as the pregnane X receptor (PXR), constitutive androstane receptor (CAR), glucocorticoid receptor (GR), and hepatic nuclear factor 4 (..
  4. Li T, Chiang J. Mechanism of rifampicin and pregnane X receptor inhibition of human cholesterol 7 alpha-hydroxylase gene transcription. Am J Physiol Gastrointest Liver Physiol. 2005;288:G74-84 pubmed
    Bile acids, steroids, and drugs activate steroid and xenobiotic receptor pregnane X receptor (PXR; NR1I2), which induces human cytochrome P4503A4 (CYP3A4) in drug metabolism and cholesterol 7 alpha-hydroxylase (CYP7A1) in bile acid ..
  5. Geick A, Eichelbaum M, Burk O. Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem. 2001;276:14581-7 pubmed
    ..Recent studies demonstrate that the nuclear receptor PXR (pregnane X receptor) is involved in xenobiotic induction of CYP3A4...
  6. Bertilsson G, Heidrich J, Svensson K, Asman M, Jendeberg L, Sydow Bäckman M, et al. Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. Proc Natl Acad Sci U S A. 1998;95:12208-13 pubmed
    ..16alpha-carbonitrile, which is a potent inducer of murine CYP3A genes and an activator of the mouse receptor PXR.1...
  7. Zucchini N, De Sousa G, Bailly Maitre B, Gugenheim J, Bars R, Lemaire G, et al. Regulation of Bcl-2 and Bcl-xL anti-apoptotic protein expression by nuclear receptor PXR in primary cultures of human and rat hepatocytes. Biochim Biophys Acta. 2005;1745:48-58 pubmed
    The pregnane X receptor (PXR) plays a major role in the protection of the body by regulating the genes involved in the metabolism and elimination of potentially toxic xeno- and endobiotics...
  8. Kurose K, Ikeda S, Koyano S, Tohkin M, Hasegawa R, Sawada J. Identification of regulatory sites in the human PXR (NR1I2) promoter region. Mol Cell Biochem. 2006;281:35-43 pubmed
    The human pregnane X receptor (hPXR, NR1I2) is a member of the nuclear receptor superfamily and a key regulator of genes encoding several major cytochrome P450 enzymes and transporters...
  9. Miura M, Satoh S, Inoue K, Kagaya H, Saito M, Inoue T, et al. Influence of CYP3A5, ABCB1 and NR1I2 polymorphisms on prednisolone pharmacokinetics in renal transplant recipients. Steroids. 2008;73:1052-9 pubmed publisher
    ..was to evaluate whether genetic polymorphisms of CYP3A5 (A6986G, CYP3A5*3), ABCB1 (C1236T, G2677T/A, C3435T) and NR1I2 (A7635G) significantly impact the pharmacokinetics of prednisolone in renal transplant recipients...
  10. Zhang J, Kuehl P, Green E, Touchman J, Watkins P, Daly A, et al. The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants. Pharmacogenetics. 2001;11:555-72 pubmed
    The pregnane X receptor (PXR)/steroid and xenobiotic receptor (SXR) transcriptionally activates cytochrome P4503A4 (CYP3A4) when ligand activated by endobiotics and xenobiotics...
  11. Watkins R, Wisely G, Moore L, Collins J, Lambert M, Williams S, et al. The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity. Science. 2001;292:2329-33 pubmed
    The human nuclear pregnane X receptor (hPXR) activates cytochrome P450-3A expression in response to a wide variety of xenobiotics and plays a critical role in mediating dangerous drug-drug interactions...
  12. Gu X, Ke S, Liu D, Sheng T, Thomas P, Rabson A, et al. Role of NF-kappaB in regulation of PXR-mediated gene expression: a mechanism for the suppression of cytochrome P-450 3A4 by proinflammatory agents. J Biol Chem. 2006;281:17882-9 pubmed
    ..of over 50% of current prescription drugs, and cyp3a4 expression is transcriptionally regulated by pregnane X receptor (PXR), which is a ligand-dependent transcription factor...
  13. Kumagai T, Suzuki H, Sasaki T, Sakaguchi S, Miyairi S, Yamazoe Y, et al. Polycyclic aromatic hydrocarbons activate CYP3A4 gene transcription through human pregnane X receptor. Drug Metab Pharmacokinet. 2012;27:200-6 pubmed
    ..Here we demonstrate that the AhR activators induce CYP3A4 through human pregnane X receptor (PXR)...
  14. Martinez A, Marquez A, Mendoza J, Taxonera C, Fernandez Arquero M, Diaz Rubio M, et al. Role of the PXR gene locus in inflammatory bowel diseases. Inflamm Bowel Dis. 2007;13:1484-7 pubmed
    The pregnane X receptor gene (PXR/NR1I2) has been recently associated with an increased risk for inflammatory bowel disease (IBD), although a subsequent case-control study failed to replicate the original association in an independent ..
  15. Iwazaki N, Kobayashi K, Morimoto K, Hirano M, Kawashima S, Furihata T, et al. Involvement of hepatocyte nuclear factor 4 alpha in transcriptional regulation of the human pregnane X receptor gene in the human liver. Drug Metab Pharmacokinet. 2008;23:59-66 pubmed
    b>Pregnane X receptor (PXR; NR1I2), a key transcriptional factor that regulates genes encoding drug-metabolizing enzymes and drug transporters, is abundantly expressed in the human liver...
  16. Wang X, Li J, Su Q, Deng X, Lu Y, Chen J, et al. A pharmacogenetic study of pregnane X receptor (NR1I2) in Han Chinese. Curr Drug Metab. 2007;8:778-86 pubmed
    The pregnane X receptor (PXR/NR1I2) gene is a critical transcriptional regulator of a number of important drug metabolizing enzymes and transporters...
  17. Fujimura T, Takahashi S, Urano T, Tanaka T, Zhang W, Azuma K, et al. Clinical significance of steroid and xenobiotic receptor and its targeted gene CYP3A4 in human prostate cancer. Cancer Sci. 2012;103:176-80 pubmed publisher
    The steroid and xenobiotic receptor (SXR) regulates cytochrome P450 (CYP) enzymes, which are key inactivators of testosterone in the liver and prostate. In the present study, we investigated SXR expression in human prostate tissues...
  18. King C, Xiao M, Yu J, Minton M, Addleman N, Van Booven D, et al. Identification of NR1I2 genetic variation using resequencing. Eur J Clin Pharmacol. 2007;63:547-54 pubmed
    The nuclear receptor NR1I2 (also called PXR or SXR) is primarily expressed in mouse and human liver and intestines...
  19. Wang X, Deng X, Chen J, Li J, Chen X, Zhao L, et al. Single nucleotide polymorphisms of the pregnane x receptor gene in Han Chinese and a comparison with other ethnic populations. Pharmacology. 2008;81:350-4 pubmed publisher
    The pregnane X receptor (PXR/NR1I2) gene is a master regulator for a number of cytochrome P450s (CYPs) and drug transporters...
  20. Siccardi M, D Avolio A, Baietto L, Gibbons S, Sciandra M, Colucci D, et al. Association of a single-nucleotide polymorphism in the pregnane X receptor (PXR 63396C-->T) with reduced concentrations of unboosted atazanavir. Clin Infect Dis. 2008;47:1222-5 pubmed publisher
    This study investigated pregnane X receptor polymorphisms in relation to unboosted atazanavir plasma concentrations in 2 cohorts of patients...
  21. Chan G, Hoque M, Cummins C, Bendayan R. Regulation of P-glycoprotein by orphan nuclear receptors in human brain microvessel endothelial cells. J Neurochem. 2011;118:163-75 pubmed publisher
    In mammalian systems, pregnane X receptor (PXR) and constitutive androstane receptor (CAR) have been recognized as xenobiotic-sensors which can up-regulate the functional expression of drug transporters, such as P-glycoprotein (P-gp)...
  22. Sookoian S, Castano G, Burgueño A, Gianotti T, Rosselli M, Pirola C. The nuclear receptor PXR gene variants are associated with liver injury in nonalcoholic fatty liver disease. Pharmacogenet Genomics. 2010;20:1-8 pubmed publisher
    To explore the contribution of gene variants and derived haplotypes of the pregnane X receptor (NR1I2) to the severity of nonalcoholic fatty liver disease (NAFLD)...
  23. Konno Y, Negishi M, Kodama S. The roles of nuclear receptors CAR and PXR in hepatic energy metabolism. Drug Metab Pharmacokinet. 2008;23:8-13 pubmed
    Nuclear receptors constitutive active/androstane receptor (CAR) and pregnane X receptor (PXR) were originally characterized as transcription factors regulating the hepatic genes that encode drug metabolizing enzymes...
  24. Mensah Osman E, Thomas D, Tabb M, Larios J, Hughes D, Giordano T, et al. Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007;109:957-65 pubmed
    ..the resistance of osteosarcoma to chemotherapy may be related to the expression of a pregnane xenobiotic receptor (PXR) variant protein and its role as the major inducer of P450 3A4 in these tumors...
  25. Li T, Chiang J. Rifampicin induction of CYP3A4 requires pregnane X receptor cross talk with hepatocyte nuclear factor 4alpha and coactivators, and suppression of small heterodimer partner gene expression. Drug Metab Dispos. 2006;34:756-64 pubmed
    Bile acids and drugs activate pregnane X receptor (PXR) to induce CYP3A4, which is the predominant cytochrome P450 enzyme expressed in the liver and intestine and plays a critical role in detoxifying bile acids and drugs, and protecting ..
  26. Xie W, Yeuh M, Radominska Pandya A, Saini S, Negishi Y, Bottroff B, et al. Control of steroid, heme, and carcinogen metabolism by nuclear pregnane X receptor and constitutive androstane receptor. Proc Natl Acad Sci U S A. 2003;100:4150-5 pubmed
    ..The orphan nuclear receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR) were originally identified as sensors able to respond to ..
  27. van de Winkel A, Menke V, Capello A, Moons L, Pot R, van Dekken H, et al. Expression, localization and polymorphisms of the nuclear receptor PXR in Barrett's esophagus and esophageal adenocarcinoma. BMC Gastroenterol. 2011;11:108 pubmed publisher
    ..In normal physiology of the gut and liver, the nuclear receptor Pregnane × Receptor (PXR) is an important factor in the detoxification of xenobiotics and bile acid homeostasis...
  28. Lamba J, Lamba V, Strom S, Venkataramanan R, Schuetz E. Novel single nucleotide polymorphisms in the promoter and intron 1 of human pregnane X receptor/NR1I2 and their association with CYP3A4 expression. Drug Metab Dispos. 2008;36:169-81 pubmed
    The hypothesis was tested that sequence diversity in pregnane X receptor (PXR) cis-regulatory regions is a significant determinant of variation in inducible and constitutive CYP3A4 expression...
  29. Xie Y, Ke S, Ouyang N, He J, Xie W, Bedford M, et al. Epigenetic regulation of transcriptional activity of pregnane X receptor by protein arginine methyltransferase 1. J Biol Chem. 2009;284:9199-205 pubmed publisher
    b>Pregnane X receptor (PXR) is a ligand-dependent transcription factor, regulating gene expression of enzymes and transporters involved in xenobiotic/drug metabolism...
  30. Sandanaraj E, Lal S, Selvarajan V, Ooi L, Wong Z, Wong N, et al. PXR pharmacogenetics: association of haplotypes with hepatic CYP3A4 and ABCB1 messenger RNA expression and doxorubicin clearance in Asian breast cancer patients. Clin Cancer Res. 2008;14:7116-26 pubmed publisher
    To characterize pregnane X receptor (PXR) polymorphic variants in healthy Asian populations [Chinese, Malay and Indian (n=100 each)], and to investigate the association between PXR haplotypes and hepatic mRNA expression of PXR and its ..
  31. Zhou J, Zhai Y, Mu Y, Gong H, Uppal H, Toma D, et al. A novel pregnane X receptor-mediated and sterol regulatory element-binding protein-independent lipogenic pathway. J Biol Chem. 2006;281:15013-20 pubmed
    The pregnane X receptor (PXR) was isolated as a xenosensor regulating xenobiotic responses. In this study, we show that PXR plays an endobiotic role by impacting lipid homeostasis...
  32. Burk O, Koch I, Raucy J, Hustert E, Eichelbaum M, Brockmoller J, et al. The induction of cytochrome P450 3A5 (CYP3A5) in the human liver and intestine is mediated by the xenobiotic sensors pregnane X receptor (PXR) and constitutively activated receptor (CAR). J Biol Chem. 2004;279:38379-85 pubmed
    ..of the mechanism involved in CYP3A5 induction revealed that constitutively activated receptor (CAR) and pregnane X receptor (PXR) transactivated the CYP3A5 promoter (-688 to +49) and that the transactivation was dependent on an ..
  33. Watkins R, Davis Searles P, Lambert M, Redinbo M. Coactivator binding promotes the specific interaction between ligand and the pregnane X receptor. J Mol Biol. 2003;331:815-28 pubmed
    The pregnane X receptor (PXR) detects the presence of a wide variety of endogenous and xenobiotic compounds, and is a master regulator of the expression of genes central to drug metabolism and excretion. We present the 2...
  34. Takami N, Sakamoto H, Yamamoto T. Steroid and xenobiotic receptor (SXR) is a key system for the acquisition of cisplatin resistance in endometrial cancer cells. J Int Med Res. 2003;31:59-68 pubmed
    A novel steroid and xenobiotic receptor (SXR) may be involved in chemoresistance, and we studied this receptor in endometrial cancer cell lines...
  35. Xie W, Barwick J, Simon C, Pierce A, Safe S, Blumberg B, et al. Reciprocal activation of xenobiotic response genes by nuclear receptors SXR/PXR and CAR. Genes Dev. 2000;14:3014-23 pubmed
    ..Nuclear receptor SXR/PXR (steroid and xenobiotic receptor/pregnenolone X receptor) has been shown both biochemically and genetically to activate CYP3A genes, ..
  36. Blumberg B, Sabbagh W, Juguilon H, Bolado J, van Meter C, Ong E, et al. SXR, a novel steroid and xenobiotic-sensing nuclear receptor. Genes Dev. 1998;12:3195-205 pubmed
    ..In support of this model, we have isolated a novel nuclear receptor, termed the steroid and xenobiotic receptor (SXR), which activates transcription in response to a diversity of natural and synthetic compounds...
  37. Johnson C, Bonzo J, Cheng J, Krausz K, Kang D, LUECKE H, et al. Cytochrome P450 regulation by ?-tocopherol in Pxr-null and PXR-humanized mice. Drug Metab Dispos. 2013;41:406-13 pubmed publisher
    The pregnane X receptor (PXR) has been postulated to play a role in the metabolism of ?-tocopherol owing to the up-regulation of hepatic cytochrome P450 (P450) 3A in human cell lines and murine models after ?-tocopherol treatment...
  38. Durdagi S, Aksoydan B, Erol I, Kantarcioglu I, Ergun Y, Bulut G, et al. Integration of multi-scale molecular modeling approaches with experiments for the in silico guided design and discovery of novel hERG-Neutral antihypertensive oxazalone and imidazolone derivatives and analysis of their potential restrictive effects o. Eur J Med Chem. 2018;145:273-290 pubmed publisher
    ..tested for their binding affinities to human AT1 receptor in radioligand binding studies, using [125I-Sar1-Ile8] AngII...
  39. JIN G, Lee J, Lee K. Chemical genetics-based development of small molecules targeting hepatitis C virus. Arch Pharm Res. 2017;40:1021-1036 pubmed publisher
    ..A number of reviews have been recently published describing the structure-activity relationship (SAR) in the development of HCV inhibitors and outlining current therapeutic approaches to hepatitis C infection...
  40. Bhattacharyya P, Mullin J, Lee B, González Martínez J, Jones S. Safety of externally stimulated intracranial electrodes during functional MRI at 1.5T. Magn Reson Imaging. 2017;38:182-188 pubmed publisher
    ..Localizer, FLASH, and GE-EPI fMRI may be safely performed in patients with a single SEEG electrode following the configurations tested in this study, but high SAR TSE scans should not be performed in these patients.
  41. Manta A, Papadopoulou D, Polyzos A, Fragopoulou A, Skouroliakou A, Thanos D, et al. Mobile-phone radiation-induced perturbation of gene-expression profiling, redox equilibrium and sporadic-apoptosis control in the ovary of Drosophila melanogaster. Fly (Austin). 2017;11:75-95 pubmed publisher
    ..four days-old adult female flies were exposed for 30 min to radiation emitted by a commercial mobile phone at a SAR of 0.15 W/kg and a SAE of 270 J/kg...
  42. Nakazaki A, Nakane Y, Ishikawa Y, Yotsu Yamashita M, Nishikawa T. Asymmetric synthesis of crambescin A-C carboxylic acids and their inhibitory activity on voltage-gated sodium channels. Org Biomol Chem. 2016;14:5304-9 pubmed publisher
    ..Structure-activity relationship (SAR) studies against voltage-gated sodium channel (VGSC) inhibition using those synthetic compounds revealed that the ..
  43. Qwebani Ogunleye T, Kolesnikova N, Steenkamp P, De Koning C, Brady D, Wellington K. A one-pot laccase-catalysed synthesis of coumestan derivatives and their anticancer activity. Bioorg Med Chem. 2017;25:1172-1182 pubmed publisher
    ..The SAR for the coumestans is similar against the melanoma UACC62 and breast MCF7 cell lines...
  44. Sidjui L, Eyong K, Hull K, Folefoc G, Leddet V, Herbette G, et al. Bioactive Seco-Lanostane-Type Triterpenoids from the Roots of Leplaea mayombensis. J Nat Prod. 2017;80:2644-2651 pubmed publisher
    ..Derivatization of the main constituent, 1, afforded the dimethyl ester 4, the monoamide 11, and diamide 12 for SAR studies...
  45. Shrestha P, Yun J, Ko Y, Yeon K, Kim D, Lee H, et al. NMR uncovers direct interaction between human NEDD4-1 and p34SEI-1. Biochem Biophys Res Commun. 2017;490:984-990 pubmed publisher
    ..We report that the WW1 domain of NEDD4-1 recognizes the SERTA domain containing the proline rich region (PRR motif) in p34SEI-1...
  46. Ji Y, Lin S, Wang Y, Su M, Zhang W, Gunosewoyo H, et al. Tying up tranylcypromine: Novel selective histone lysine specific demethylase 1 (LSD1) inhibitors. Eur J Med Chem. 2017;141:101-112 pubmed publisher
    ..In this study, we present the SAR data for a novel series of conformationally-restricted TCP-based LSD1 inhibitors, both in their racemic and ..
  47. Poynter S, Lisser G, Monjo A, DeWitte Orr S. Sensors of Infection: Viral Nucleic Acid PRRs in Fish. Biology (Basel). 2015;4:460-93 pubmed publisher
    ..It also discusses what is currently known of the downstream signaling molecules for each PRR family and the resulting antiviral response, either type I interferons (IFNs) or pro-inflammatory cytokine ..
  48. Zhou Y, Wang X, Li H, Zhang J, Chen Z, Xie W, et al. Polymorphisms of ABCG2, ABCB1 and HNF4α are associated with Lamotrigine trough concentrations in epilepsy patients. Drug Metab Pharmacokinet. 2015;30:282-7 pubmed publisher
    ..nucleotide polymorphisms (SNPs) involved in LTG metabolism and transport pathways, including UGT2B7, ABCB1, ABCG2, NR1I2 and HNF4α were genotyped in 140 Chinese epilepsy patients...
  49. Charles M, Brookfield J, Ekwuru T, Stockley M, Dunn J, Riddick M, et al. Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties. J Med Chem. 2015;58:8309-13 pubmed publisher
    ..Scaffold hopping and subsequent SAR directed development led to a series of low nanomolar inhibitors of LIMK1 and LIMK2 that also inhibited the direct ..
  50. Tocchetti G, Rigalli J, Arana M, Villanueva S, Mottino A. Modulation of expression and activity of intestinal multidrug resistance-associated protein 2 by xenobiotics. Toxicol Appl Pharmacol. 2016;303:45-57 pubmed publisher
    ..Transcriptional regulation is usually mediated by a group of nuclear receptors. The pregnane X receptor (PXR) is a major member of this group...
  51. Witte D, Zeeh F, Gädeken T, Gieseler F, Rauch B, Settmacher U, et al. Proteinase-Activated Receptor 2 Is a Novel Regulator of TGF-β Signaling in Pancreatic Cancer. J Clin Med. 2016;5: pubmed
    ..We have recently identified PAR2 as a factor required for TGF-β1-dependent cell motility in ductal pancreatic adenocarcinoma (PDAC) cells...
  52. Osokogu O, Dodd C, Pacurariu A, Kaguelidou F, Weibel D, Sturkenboom M. Drug Safety Monitoring in Children: Performance of Signal Detection Algorithms and Impact of Age Stratification. Drug Saf. 2016;39:873-81 pubmed publisher
    ..We tested the performance of two established SDAs: the proportional reporting ratio (PRR) and the empirical Bayes geometric mean (EBGM) on a pediatric dataset from FAERS (2004-2012)...
  53. Huang W, Zhang Z, Ranade R, Gillespie J, Barros Álvarez X, Creason S, et al. Optimization of a binding fragment targeting the "enlarged methionine pocket" leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors. Bioorg Med Chem Lett. 2017;27:2702-2707 pubmed publisher
    ..To further improve cellular potency, SAR investigation of a binding fragment targeting the "enlarged methionine pocket" (EMP) was performed...
  54. Taha M, Ismail N, Imran S, Rahim F, Wadood A, Al Muqarrabun L, et al. In silico binding analysis and SAR elucidations of newly designed benzopyrazine analogs as potent inhibitors of thymidine phosphorylase. Bioorg Chem. 2016;68:80-9 pubmed publisher
    ..Current studies have revealed that these compounds established stronger hydrogen bonding networks with active site residues as compare to the standard compound 7DX. ..
  55. Megías J, Martínez A, Yáñez A, Goodridge H, Gozalbo D, Gil M. TLR2, TLR4 and Dectin-1 signalling in hematopoietic stem and progenitor cells determines the antifungal phenotype of the macrophages they produce. Microbes Infect. 2016;18:354-63 pubmed publisher
    ..cells) were cultured with M-CSF to induce macrophage differentiation, in the presence or absence of the following PRR agonists: Pam3CSK4 (TLR2 ligand), LPS (TLR4 ligand), depleted zymosan (which only activates Dectin-1), or C...
  56. Alvarez Arce A, Lee Rivera I, Lopez E, Hernandez Cruz A, López Colomé A. Thrombin-Induced Calpain Activation Promotes Protease-Activated Receptor 1 Internalization. Int J Cell Biol. 2017;2017:1908310 pubmed publisher
    ..Four members of this family have been identified: PAR1-4...
  57. Matsuo K, Ross M, Yunokawa M, Johnson M, Machida H, Omatsu K, et al. Salvage chemotherapy with taxane and platinum for women with recurrent uterine carcinosarcoma. Gynecol Oncol. 2017;147:565-571 pubmed publisher
    To examine survival after recurrence (SAR) among women with recurrent uterine carcinosarcoma who received a taxane/platinum doublet as the first-line salvage chemotherapy.
  58. Jiang F, Guo A, Xu J, Wang H, Mo X, You Q, et al. Identification and optimization of novel 6-acylamino-2-aminoquinolines as potent Hsp90 C-terminal inhibitors. Eur J Med Chem. 2017;141:1-14 pubmed publisher
    ..Compound 13 was identified as the lead compound and then systematical structure activity relationship (SAR) study was conducted...
  59. Zhang T, Li S, Yuan W, Zhang Y, Meng F. Design, synthesis and molecular docking studies of N-(9,10-anthraquinone-2-carbonyl)amino acid derivatives as xanthine oxidase inhibitors. Chem Biol Drug Des. 2017;: pubmed publisher
    ..1 ?M). Preliminary SAR analysis pointed that an aromatic amino acid fragment, e.g...
  60. Kumari P, Saha I, Narayanan A, Narayanan S, Takaoka A, Kumar N, et al. Essential role of HCMV deubiquitinase in promoting oncogenesis by targeting anti-viral innate immune signaling pathways. Cell Death Dis. 2017;8:e3078 pubmed publisher
    ..Furthermore, HCMV deubiquitinase acquires pro-tumor functions by inhibiting PRR-mediated type I interferon via deubiquitination of TRAF6, TRAF3, IRAK1, IRF7 and STING...
  61. Subeesh V, Singh H, Maheswari E, Beulah E. Novel adverse events of vortioxetine: A disproportionality analysis in USFDA adverse event reporting system database. Asian J Psychiatr. 2017;30:152-156 pubmed publisher
    ..Most commonly used three data mining algorithms, Reporting Odds Ratio (ROR), Proportional Reporting Ratio (PRR) and Information Component (IC) were selected for the study and they were applied retrospectively in USFDA AERS ..
  62. Guan D, Chen F, Xiong L, Tang F, Faridoon F, Qiu Y, et al. Extra sugar on vancomycin: new analogues for combating multidrug-resistant Staphylococcus aureus and vancomycin-resistant Enterococci. J Med Chem. 2017;: pubmed publisher
    ..various sugar moieties on the 7th-amino acid phenyl ring and lipophilic substitutions on vancosamine with extensive SAR analysis...
  63. Lolodi O, Wang Y, Wright W, Chen T. Differential Regulation of CYP3A4 and CYP3A5 and Its Implication in Drug Discovery. Curr Drug Metab. 2017;: pubmed publisher
    ..Such components include the pregnane X receptor (PXR) and the cytochrome P450 (CYP) 3A4 and 3A5 enzymes...
  64. Oleson L, von Moltke L, Greenblatt D, Court M. Identification of polymorphisms in the 3'-untranslated region of the human pregnane X receptor (PXR) gene associated with variability in cytochrome P450 3A (CYP3A) metabolism. Xenobiotica. 2010;40:146-62 pubmed publisher
    Single nucleotide polymorphisms in the 3'-untranslated region (3'UTR) of the human pregnane X receptor (PXR) gene might contribute to interindividual variability in cytochrome P450 3A (CYP3A) activity...
  65. Han N, Shi L, Guo Q, Sun W, Yu Y, Yang L, et al. HAT1 induces lung cancer cell apoptosis via up regulating Fas. Oncotarget. 2017;8:89970-89977 pubmed publisher
    ..We observed that the expression of Fas was negatively correlated with PAR2 in LCCs. Activation of PAR2 suppressed the expression of Fas in normal lung epithelial cells...
  66. Furuhama A, Hayashi T, Yamamoto H, Tatarazako N. External validation of acute-to-chronic models for estimation of reproductive toxicity to Daphnia magna. SAR QSAR Environ Res. 2017;28:765-781 pubmed publisher
    ..and applicability of previously proposed models for the reproductive toxicity of chemicals to Daphnia magna [SAR QSAR Environ. Res...
  67. Yang J, Hao C, Yang D, Shi D, Song X, Luan X, et al. Pregnane X receptor is required for interleukin-6-mediated down-regulation of cytochrome P450 3A4 in human hepatocytes. Toxicol Lett. 2010;197:219-26 pubmed publisher
    ..Meanwhile, the repression of CYP3A4 by IL-6 occurred after the decrease of pregnane X receptor (PXR) in human hepatocytes...
  68. Chen I, Velicer G, Yu Y. Divergence of functional effects among bacterial sRNA paralogs. BMC Evol Biol. 2017;17:199 pubmed publisher
    ..The sRNA Pxr functions as a developmental gatekeeper in the model cooperative bacterium Myxococcus xanthus...
  69. Rahmouni A, Souiei S, Belkacem M, Romdhane A, Bouajila J, Ben Jannet H. Synthesis and biological evaluation of novel pyrazolopyrimidines derivatives as anticancer and anti-5-lipoxygenase agents. Bioorg Chem. 2016;66:160-8 pubmed publisher
    ..Compounds were screened for their cytotoxic (HCT-116 and MCF-7) and 5-lipoxygenase inhibition activities. The structure-activity relationship (SAR) was discussed.