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The Human Nuclear Xenobiotic Receptor PXR: Structural Determinants of Directed Promiscuity
Abstract
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. We present the crystal structures of the ligand-binding domain of hPXR both alone and in complex with the cholesterol-lowering drug SR12813 at resolutions of 2.5 and 2.75 angstroms, respectively. The hydrophobic ligand-binding cavity of hPXR contains a small number of polar residues, permitting SR12813 to bind in three distinct orientations. The position and nature of these polar residues were found to be critical for establishing the precise pharmacologic activation profile of PXR. Our findings provide important insights into how hPXR detects xenobiotics and may prove useful in predicting and avoiding drug-drug interactions.
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Cited by
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Structure of P-Glycoprotein Reveals a Molecular Basis for Poly-Specific Drug Binding
Aller, S. G., Yu, J., Ward, A., Weng, Y., Chittaboina, S., Zhuo, R., Harrell, P. M., Trinh, Y. T., Zhang, Q., Urbatsch, I. L., et al. (2009) · Science · doi:10.1126/science.1168750 · Cited by 1,929
Venkatesh, M., Mukherjee, S., Wang, H., Li, H., Sun, K., Benechet, A. P., Qiu, Z., Maher, L., Redinbo, M. R., Phillips, R. S., et al. (2014) · Immunity · doi:10.1016/j.immuni.2014.06.014 · Cited by 1,066
Self-citationImplications of protein flexibility for drug discovery
Teague, S. J. (2003) · Nature Reviews Drug Discovery · doi:10.1038/nrd1129 · Cited by 755
Leesnitzer, L. M., Parks, D. J., Bledsoe, R. K., Cobb, J. E., Collins, J. L., Consler, T. G., Davis, R. G., Hull-Ryde, E. A., Lenhard, J. M., Patel, L., et al. (2002) · Biochemistry · doi:10.1021/bi0159581 · Cited by 566
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Metadata
- Authors
- Watkins, R. E., Wisely, G. B., Moore, L. B., Collins, J. L., Lambert, M. H., Williams, S. P., Willson, T. M., Kliewer, S. A., & Redinbo, M. R.
- Venue
- Science
- Published
- 2001-06-22
- Volume
- 292
- Issue
- 5525
- Pages
- 2329-2333
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W1981873124
- Cited by
- 760
- References
- 0
- FWCI
- 22.25
- Type
- journal article
- Language
- en
- Open access
- closed
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- Watkins, R. E., Wisely, G. B., Moore, L. B., Collins, J. L., Lambert, M. H., Williams, S. P., Willson, T. M., Kliewer, S. A., & Redinbo, M. R. (2001). The Human Nuclear Xenobiotic Receptor PXR: Structural Determinants of Directed Promiscuity. Science. https://doi.org/10.1126/science.1060762
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