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Pregnane X-Receptor

Chang TKH, Waxman DJ (2006) Synthetic drugs and natural products as modulators of constitutive androstane receptor (CAR) and pregnane X receptor (PXR). Drug Metab Rev 38 51-73... [Pg.893]

Coghlan MJ, Carroll WA, Gopalaknshnan M (2001) Recent developments in the biology and medicinal chemistry of potassium channel modulators update from a decade of progress. JMed Chem 44 1627-1653 Pregnane X Receptor... [Pg.998]

Potassium Competitive Acid Blockers The pregnane X receptor (PXR) is a promiscuous nuclear receptor, that has evolved to protect the body from toxic chemicals. It is activated by a wide variety of xenobiotics including several diugs like rifampicin, hyperforin ( the active ingredient of St. John s wort), clotrimazole and others. PXR heterodimerizes with the... [Pg.998]

Pregnane X Receptor, Nuclear Receptor Regulation of Drug-metabolizing P450-Enzymes. [Pg.1054]

The retinoid X receptor (RXR) is a nuclear receptor that binds and is activated by certain endogenous retinoids, such as 9-cis-retinoic acid. RXR is the obligatory heterodimerization partner for a large number of nonclassic steroid nuclear receptors, such as thyroid hoimone receptor, vitamin D3 receptor, peroxisome proliferator-activated receptor and pregnane X receptor. [Pg.1071]

Gene regulation by tocopherols has mainly been associated with PKC because of its deactivation by a-tocopherol and its contribution in the regulation of a number of transcription factors (NF-kappaB, API). A direct participation of the pregnane X receptor (PXR)/ retinoid X receptor (RXR) has been also shown. The antioxidant-responsive element (ARE) and the TGF-beta-responsive element appear in some cases to be implicated as well. The obser ved immunmodulatory function of a-tocopherol may also be attributed to the fact that the release of the proinflammatory cytokine interlukin-l 3 can be inhibited by a-tocopherol via... [Pg.1296]

Ekins S, Erickson JA. A pharmacophore for human pregnane X-receptor ligands. Drug Metab Dispos 2002 30 96-9. [Pg.375]

Ruhl, R. et al.. Carotenoids and their metabolites are naturally occurring activators of gene expression via the pregnane X receptor. Fur. J. Nutr, 43, 336, 2004. [Pg.192]

A different pharmacophore [74], containing only one H-bond acceptor was suggested for the interaction of drugs with the transcriptional regulator PXR (pregnane X receptor) [75]. [Pg.475]

Hustert, E., et al., "Natural Protein Variants of Pregnane X Receptor with Altered Transactivation Activity Toward CYP3A4," Drug Metab. Dispos., 29, 1454—1459 (2001). [Pg.56]

Yang D, Wang X, Chen Y, Deng R, Yan B (2009) Pyrethroid insecticides isoform-dependent hydrolysis, induction of cytochrome P450 3A4 and evidence on the involvement of the pregnane X receptor. Toxicol Appl Pharmacol 237 49-58... [Pg.133]

Xie, W., Yeuh, M.F., Radominska-Pandya, A., Saini, S.P., Negishi, Y., Bottroff, B.S., Cabrera, G.Y., Tukey, R.H. and Evans, R.M. (2003) Control of steroid, heme, and carcinogen metabolism by nuclear pregnane X receptor and constitutive androstane receptor. Proceedings... [Pg.312]

Chen, C., Staudinger, J.L. and Klaassen, C.D. (2003) Nuclear receptor, pregnane X receptor, is required for induction of UDP-glucuronosyltransferases in mouse liver by pregnenolone-16 alpha-carbonitrile. Drug Metabolism and Disposition, 31, 908—915. [Pg.312]

Rosenfeld, J.M., Vargas, R., Jr, Xie, W. and Evans, R.M. (2003) Genetic profiling defines the xenobiotic gene network controlled by the nuclear receptor pregnane X receptor. Molecular Endocrinology, 17, 1268-1282. [Pg.313]

Kast, H.R., Goodwin, B., Tarr, P.T., Jones, S.A., Anisfeld, A.M., Stoltz, C.M., Tontonoz, P., Kliewer, S., Willson, T.M. and Edwards, P.A. (2002) Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor. Journal of Biological Chemistry, 277, 2908-2915. [Pg.313]

Teng, S., Jekerle, V. and Piquette-Miller, M. (2003) Induction of ABCC3 (MRP3) by pregnane X receptor activators. Drug Metabolism and Disposition, 31,1296-1299. [Pg.313]

Sinz, M., Kim, S., Zhu, Z., Chen, T., Anthony, M., Dickinson, K. and Rodrigues, A.D. (2006) Evaluation of 170 xenobiotics as transactivators of human pregnane X receptor (hPXR) and correlation to known CYP3A4 drug interactions. Current Drug Metabolism, 7, 375-388. [Pg.314]

Moore, L.B., Goodwin, B., Jones, S.A., Wisely, G.B., Serabjit-Singh, C.J., Willson, T.M., Collins, J.L. and Kliewer, S. A. (2000) St. John s wort induces hepatic drug metabolism through activation of the pregnane X receptor. Proceedings of the National Academy of Sciences of the United States of America, 97, 7500-7502. [Pg.314]

Stedman, C.A., Hddle, C., Coulter, S.A., Sonoda, J., Alvarez, J.G., Moore, D.D., Evans, R.M. and Downes, M. (2005) Nuclear receptors constitutive androstane receptor and pregnane X receptor ameliorate cholestatic liver injury. Proceedings of the National Academy of Sciences of the United States of America, 102, 2063-2068. [Pg.314]

Activation of pregnane X receptor disrupts glucocorticoid and mineralocorticoid homeostasis. [Pg.315]

Zhou, J., Zhai, Y., Mu, Y Gong, H., Uppal, H., Toma, D., Ren, S., Evans, R.M. and Xie, W. (2006) A novel pregnane X receptor-mediated and sterol regulatory element-hinding protein-independent lipogenic pathway. Journal of Biological Chemistry, 281, 15013—15020. [Pg.315]

P450 Inducers Acting via Nuclear Receptors 14.2.3.1 Pregnane X Receptor... [Pg.322]

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Human pregnane-X-receptor

PXR, Pregnane X receptor

Pregnan

Pregnane

Pregnane X receptor ligands

Receptors X receptor

Receptors pregnane X receptor

Receptors pregnane X receptor

The Pregnane X Receptor

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