Human pregnane-X-receptor

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

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. 

Kobayashi, K., Yamagami, S., Higuchi, T., Hosokawa, M. and Chiba, K. (2004) Key structural features of ligands for activation of human pregnane X receptor. Drug Metabolism and Disposition The Biological Fate of Chemicals, 32, 468-472. 

Watkins RE, Noble SM, Redinbo MR (2002) Structural insights into the promiscuity and function of the human pregnane X receptor. Curr Opin Drug Discov Devel 5 150-158... 

Koyano, S., Kurose, K., Saito, Y., et al. (2004) Functional characterization of four naturally occurring variants of human pregnane X receptor (PXR) one variant causes dramatic loss of both DNA binding activity and the transactivation of the CYP3A4 promoter/enhancer region. Drug Metab. Dispos. 32, 149-154. 

Figure 9.10 Illustration depicting DNA elements found in CYP3A genes and the activation of the human pregnane X receptor (PXR) by ligand (RIF) and subsequent transcriptional activation of CYP3A4 gene by the PXR/RXR heterodimer. dNR-1-3, nuclear receptors 1, 2, and 3, respectively PXR, pregnane X receptor RXR, retinoid X receptor RIF, rifampicin SRC-1, steroid receptor co-activator XREM, xenobiotic responsive enhancer module.

Chrencik JE, et al. Structural disorder in the complex of human pregnane X receptor and the macrolide antibiotic rifampicin. 

Goodwin B, Hodgson E, Liddle C. The orphan human pregnane X receptor mediates the transcription activation of CYP3A4 by rifampicin through a distal enhancer module. Mol Pharmacol 1999 56 1329-39. 

Scheer N, Ross J, Rode A, et al. A novel panel of mouse models to evaluate the role of human pregnane X receptor and constitutive androstane receptor in drug response. / Clin Invest. 2008 118 3228-3239. 

Zhang J, Kuehl P, Green ED, Touchman JW, Watkins PB, et al. 2001. The human pregnane X receptor genomic structure and identification and functional characterization of natural allelic variants. Pharmacogenetics 11 555-72... 

Faucette SR, Zhang TC, Moore R, Sueyoshi T, Omiecinski C, LeCluyse EL, et al. Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. J Pharmacol Exp Ther 2007 320 72-80. 

Chrencik JE, Orans JO, Moore LB, Xue Y, Peng L, Collins JL, et al. Structural disorder in the complex of human pregnane X receptor and the macrolide antibiotic rifampicin. Mol Endocrinol 2005 19 1125-34. 

Jacobs MN, Dickins M, Lewis DF. Homology modelling of the nuclear receptors Human oestrogen receptorbeta (hERbeta), the human pregnane-X-receptor... 

He, P., Court, M.H., Greenblatt, D.J. and von Molfke, L.L. (2006) Human pregnane X receptor genetic polymorphisms, alternative mRNA splice variants, and cytochrome P450 3A metabolic activity. Journal of Clinical Pharmacology, 46, 1356-1369. 

Bauer, B., Yang, X., Hartz, A. M., Olson, E. R., Zhao, R., Kalvass, J. C., Pollack, G. M., and Miller, D. S. (2006) In vivo activation of human pregnane X receptor tightens the blood-brain-barrier to methadone through P-glycoprotein up-regulation. Mol. Pharmacol. 70, 1212-1219. 

Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug Metab. Dispos. 29, 1325-1331. 

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