• 51701 Citations
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1986 …2020

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Article
2008

Structural basis of human pregnane X receptor activation by the hops constituent colupulone

Teotico, D. G., Bischof, J. J., Peng, L., Kliewer, S. A. & Redinbo, M. R., Dec 1 2008, In : Molecular Pharmacology. 74, 6, p. 1512-1520 9 p.

Research output: Contribution to journalArticle

49 Scopus citations
2007

Crystal structure of the pregnane X receptor-estradiol complex provides insights into endobiotic recognition

Xue, Y., Moore, L. B., Orans, J., Peng, L., Bencharit, S., Kliewer, S. A. & Redinbo, M. R., May 1 2007, In : Molecular Endocrinology. 21, 5, p. 1028-1038 11 p.

Research output: Contribution to journalArticle

74 Scopus citations

Differential regulation of bile acid homeostasis by the farnesoid X receptor in liver and intestine

Kim, I., Ahn, S. H., Inagaki, T., Choi, M., Ito, S., Guo, G. L., Kliewer, S. A. & Gonzalez, F. J., Dec 1 2007, In : Journal of lipid research. 48, 12, p. 2664-2672 9 p.

Research output: Contribution to journalArticle

315 Scopus citations

Endocrine Regulation of the Fasting Response by PPARα-Mediated Induction of Fibroblast Growth Factor 21

Inagaki, T., Dutchak, P., Zhao, G., Ding, X., Gautron, L., Parameswara, V., Li, Y., Goetz, R., Mohammadi, M., Esser, V., Elmquist, J. K., Gerard, R. D., Burgess, S. C., Hammer, R. E., Mangelsdorf, D. J. & Kliewer, S. A., Jun 6 2007, In : Cell Metabolism. 5, 6, p. 415-425 11 p.

Research output: Contribution to journalArticle

939 Scopus citations

FXR agonists and FGF15 reduce fecal bile acid excretion in a mouse model of bile acid malabsorption

Jung, D., Inagaki, T., Gerard, R. D., Dawson, P. A., Kliewer, S. A., Mangelsdorf, D. J. & Moschetta, A., Dec 1 2007, In : Journal of lipid research. 48, 12, p. 2693-2700 8 p.

Research output: Contribution to journalArticle

86 Scopus citations

Molecular insights into the Klotho-dependent, endocrine mode of action of fibroblast growth factor 19 subfamily members

Goetz, R., Beenken, A., Ibrahimi, O. A., Kalinina, J., Olsen, S. K., Eliseenkova, A. V., Xu, C., Neubert, T. A., Zhang, F., Linhardt, R. J., Yu, X., White, K. E., Inagaki, T., Kliewer, S. A., Yamamoto, M., Kurosu, H., Ogawa, Y., Kuro-o, M., Lanske, B., Razzaque, M. S. & 1 others, Mohammadi, M., May 1 2007, In : Molecular and cellular biology. 27, 9, p. 3417-3428 12 p.

Research output: Contribution to journalArticle

335 Scopus citations

Tissue-specific expression of βklotho and Fibroblast Growth Factor (FGF) receptor isoforms determines metabolic activity of FGF19 and FGF21

Kurosu, H., Choi, M., Ogawa, Y., Dickson, A. S., Goetz, R., Eliseenkova, A. V., Mohammadi, M., Rosenblatt, K. P., Kliewer, S. A. & Kuro-O, M., Sep 14 2007, In : Journal of Biological Chemistry. 282, 37, p. 26687-26695 9 p.

Research output: Contribution to journalArticle

464 Scopus citations
2006

Identification of a hormonal basis for gallbladder filling

Choi, M., Moschetta, A., Bookout, A. L., Peng, L., Umetani, M., Holmstrom, S. R., Suino-Powell, K., Xu, H. E., Richardson, J. A., Gerard, R. D., Mangelsdorf, D. J. & Kliewer, S. A., Nov 1 2006, In : Nature medicine. 12, 11, p. 1253-1255 3 p.

Research output: Contribution to journalArticle

192 Scopus citations

Regulation of antibacterial defense in the small intestine by the nuclear bile acid receptor

Inagaki, T., Moschetta, A., Lee, Y. K., Peng, L., Zhao, G., Downes, M., Yu, R. T., Shelton, J. M., Richardson, J. A., Repa, J. J., Mangelsdorf, D. J. & Kliewer, S. A., Mar 7 2006, In : Proceedings of the National Academy of Sciences of the United States of America. 103, 10, p. 3920-3925 6 p.

Research output: Contribution to journalArticle

560 Scopus citations
2005

Crystallographic identification and functional characterization of phospholipids as ligands for the orphan nuclear receptor steroidogenic factor-1

Li, Y., Choi, M., Cavey, G., Daugherty, J., Suino, K., Kovach, A., Bingham, N. C., Kliewer, S. A. & Xu, H. E., Feb 18 2005, In : Molecular cell. 17, 4, p. 491-502 12 p.

Research output: Contribution to journalArticle

178 Scopus citations

Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis

Inagaki, T., Choi, M., Moschetta, A., Peng, L., Cummins, C. L., McDonald, J. G., Luo, G., Jones, S. A., Goodwin, B., Richardson, J. A., Gerard, R. D., Repa, J. J., Mangelsdorf, D. J. & Kliewer, S. A., Oct 1 2005, In : Cell Metabolism. 2, 4, p. 217-225 9 p.

Research output: Contribution to journalArticle

1043 Scopus citations

Orphan nuclear receptor LRH-1 is required to maintain Oct4 expression at the epiblast stage of embryonic development

Gu, P., Goodwin, B., Chung, A. C. K., Xu, X., Wheeler, D. A., Price, R. R., Galardi, C., Peng, L., Latour, A. M., Koller, B. H., Gossen, J., Kliewer, S. A. & Cooney, A. J., May 2005, In : Molecular and cellular biology. 25, 9, p. 3492-3505 14 p.

Research output: Contribution to journalArticle

212 Scopus citations

Pregnane X receptor: Predicting and preventing drug interactions

Kliewer, S. A., Nov 18 2005, In : Thrombosis research. 117, 1-2, p. 133-136 4 p.

Research output: Contribution to journalArticle

6 Scopus citations

Structural and biochemical basis for selective repression of the orphan nuclear receptor liver receptor homolog 1 by small heterodimer partner

Li, Y., Choi, M., Suino, K., Kovach, A., Daugherty, J., Kliewer, S. A. & Xu, H. E., Jul 5 2005, In : Proceedings of the National Academy of Sciences of the United States of America. 102, 27, p. 9505-9510 6 p.

Research output: Contribution to journalArticle

82 Scopus citations

Structural disorder in the complex of human pregnane X receptor and the macrolide antibiotic rifampicin

Chrencik, J. E., Orans, J., Moore, L. B., Xue, Y., Peng, L., Collins, J. L., Wisely, G. B., Lambert, M. H., Kliewer, S. A. & Redinbo, M. R., May 1 2005, In : Molecular Endocrinology. 19, 5, p. 1125-1134 10 p.

Research output: Contribution to journalArticle

156 Scopus citations
2004

Enhanced acetaminophen toxicity by activation of the pregnane X receptor

Guo, G. L., Moffit, J. S., Nicol, C. J., Ward, J. M., Aleksunes, L. A., Slitt, A. L., Kliewer, S. A., Manautou, J. E. & Gonzalez, F. J., Dec 1 2004, In : Toxicological Sciences. 82, 2, p. 374-380 7 p.

Research output: Contribution to journalArticle

83 Scopus citations

The nuclear xenobiotic receptor CAR: Structural determinants of constitutive activation and heterodimerization

Suino, K., Peng, L., Reynolds, R., Li, Y., Cha, J. Y., Repa, J. J., Kliewer, S. A. & Xu, H. E., Dec 22 2004, In : Molecular cell. 16, 6, p. 893-905 13 p.

Research output: Contribution to journalArticle

163 Scopus citations
2003

2.1 Å crystal structure of human PXR in complex with the St. John's wort compound hyperforin

Watkins, R. E., Maglich, J. M., Moore, L. B., Wisely, G. B., Noble, S. M., Davis-Searles, P. R., Lambert, M. H., Kliewer, S. A. & Redinbo, M. R., Feb 18 2003, In : Biochemistry. 42, 6, p. 1430-1438 9 p.

Research output: Contribution to journalArticle

280 Scopus citations

Complementary Roles of Farnesoid X Receptor, Pregnane X Receptor, and Constitutive Androstane Receptor in Protection against Bile Acid Toxicity

Guo, G. L., Lambert, G., Negishi, M., Ward, J. M., Brewer, H. B., Kliewer, S. A., Gonzalez, F. J. & Sinal, C. J., Nov 14 2003, In : Journal of Biological Chemistry. 278, 46, p. 45062-45071 10 p.

Research output: Contribution to journalArticle

239 Scopus citations

CYP3A induction by N-hydroxyformamide tumor necrosis factor-α converting enzyme/matrix metalloproteinase inhibitors: Use of a pregnane X receptor activation assay and primary hepatocyte culture for assessing induction potential in humans

Tippin, T. K., Hamilton, G., Moore, L., Beaudet, E. J., Jolley, S., Brodie, T. A., Andrews, R. C., Becherer, J. D., McDougald, D. L., Gaul, M. D., Hoivik, D. J., Mellon-Kusibab, K., Lehmann, J., Kliewer, S., Novick, S., Laethem, R., Zhao, Z. & LeCluyse, E. L., Jul 1 2003, In : Drug Metabolism and Disposition. 31, 7, p. 870-877 8 p.

Research output: Contribution to journalArticle

8 Scopus citations

Definition of a novel growth factor-dependent signal cascade for the suppression of bile acid biosynthesis

Holt, J. A., Luo, G., Billin, A. N., Bisi, J., McNeill, Y. Y., Kozarsky, K. F., Donahee, M., Wang, D. Y., Mansfield, T. A., Kliewer, S. A., Goodwin, B. & Jones, S. A., Jul 1 2003, In : Genes and Development. 17, 13, p. 1581-1591 11 p.

Research output: Contribution to journalArticle

467 Scopus citations

Differential regulation of rat and human CYP7A 1 by the nuclear oxysterol receptor liver X receptor-α

Goodwin, B., Watson, M. A., Kim, H., Miao, J., Kemper, J. K. & Kliewer, S. A., Mar 1 2003, In : Molecular Endocrinology. 17, 3, p. 386-394 9 p.

Research output: Contribution to journalArticle

148 Scopus citations

Functional and structural comparison of PXR and CAR

Moore, J. T., Moore, L. B., Maglich, J. M. & Kliewer, S. A., Feb 17 2003, In : Biochimica et Biophysica Acta - General Subjects. 1619, 3, p. 235-238 4 p.

Research output: Contribution to journalArticle

97 Scopus citations

Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis

Liu, Y., Binz, J., Numerick, M. J., Dennis, S., Luo, G., Desai, B., MacKenzie, K. I., Mansfield, T. A., Kliewer, S. A., Goodwin, B. & Jones, S. A., Dec 2003, In : Journal of Clinical Investigation. 112, 11, p. 1678-1687 10 p.

Research output: Contribution to journalArticle

Open Access
314 Scopus citations

Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes

Maglich, J. M., Parks, D. J., Moore, L. B., Collins, J. L., Goodwin, B., Billin, A. N., Stoltz, C. A., Kliewer, S. A., Lambert, M. H., Willson, T. M. & Moore, J. T., May 9 2003, In : Journal of Biological Chemistry. 278, 19, p. 17277-17283 7 p.

Research output: Contribution to journalArticle

334 Scopus citations

Identification of bile acid precursors as endogenous ligands for the nuclear xenobiotic pregnane X receptor

Goodwin, B., Gauthier, K. C., Umetani, M., Watson, M. A., Lochansky, M. I., Collins, J. L., Leitersdorf, E., Mangelsdorf, D. J., Kliewer, S. A. & Repa, J. J., Jan 7 2003, In : Proceedings of the National Academy of Sciences of the United States of America. 100, 1, p. 223-228 6 p.

Research output: Contribution to journalArticle

162 Scopus citations

The nuclear pregnane X receptor regulates xenobiotic detoxification

Kliewer, S. A., Jul 1 2003, In : Journal of Nutrition. 133, 7 SUPPL., p. 2444S-2447S

Research output: Contribution to journalArticle

126 Scopus citations
2002

Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines

Collins, J. L., Binz, J. G., Plunket, K. D., Morgan, D. G., Beaudet, E. J., Whitney, K. D., Kliewer, S. A., Willson, T. M., Fivush, A. M., Watson, M. A., Galardi, C. M., Lewis, M. C., Moore, L. B., Parks, D. J., Wilson, J. G. & Tippin, T. K., May 9 2002, In : Journal of Medicinal Chemistry. 45, 10, p. 1963-1966 4 p.

Research output: Contribution to journalArticle

334 Scopus citations

Nuclear pregnane X receptor and constitutive androstane receptor regulate overlapping but distinct sets of genes involved in xenobiotic detoxification

Maglich, J. M., Stoltz, C. M., Goodwin, B., Hawkins-Brown, D., Moore, J. T. & Kliewer, S. A., Sep 1 2002, In : Molecular Pharmacology. 62, 3, p. 638-646 9 p.

Research output: Contribution to journalArticle

549 Scopus citations

Nuclear receptors I. Nuclear receptors and bile acid homeostasis

Goodwin, B. & Kliewer, S. A., 2002, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 282, 6 45-6, p. G926-G931

Research output: Contribution to journalArticle

54 Scopus citations

Peroxisome proliferator-activated receptors and reverse endocrinology

Kliewer, S. & Kline, G. S., Jan 1 2002, In : Pharmacochemistry Library. 32, C, p. 67-79 13 p.

Research output: Contribution to journalArticle

Peroxisome proliferator-activated receptor-α regulates fatty acid utilization in primary human skeletal muscle cells

Muoio, D. M., Way, J. M., Tanner, C. J., Winegar, D. A., Kliewer, S. A., Houmard, J. A., Kraus, W. E. & Lynis Dohm, G., Jan 1 2002, In : Diabetes. 51, 4, p. 901-909 9 p.

Research output: Contribution to journalArticle

Open Access
174 Scopus citations

Pregnane X receptor (PXR), constitutive androstane receptor (CAR), and benzoate X receptor (BXR) define three pharmacologically distinct classes of nuclear receptors

Moore, L. B., Maglich, J. M., McKee, D. D., Wisely, B., Willson, T. M., Kliewer, S. A., Lambert, M. H. & Moore, J. T., 2002, In : Molecular Endocrinology. 16, 5, p. 977-986 10 p.

Research output: Contribution to journalArticle

Open Access
290 Scopus citations

Regulation of cholesterol homeostasis by the liver X receptors in the central nervous system

Whitney, K. D., Watson, M. A., Collins, J. L., Benson, W. G., Stone, T. M., Numerick, M. J., Tippin, T. K., Wilson, J. G., Winegar, D. A. & Kliewer, S. A., 2002, In : Molecular Endocrinology. 16, 6, p. 1378-1385 8 p.

Research output: Contribution to journalArticle

164 Scopus citations

Regulation of cholesterol homeostasis by the liver X receptors in the central nervous system

Whitney, K. D., Watson, M. A., Collins, J. L., Benson, W. G., Stone, T. M., Numerick, M. J., Tippin, T. K., Wilson, J. G., Winegar, D. A. & Kliewer, S. A., 2002, In : Molecular Endocrinology. 16, 6, p. 1378-1385 8 p.

Research output: Contribution to journalArticle

Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor

Kast, H. R., Goodwin, B., Tarr, P. T., Jones, S. A., Anisfeld, A. M., Stoltz, C. M., Tontonoz, P., Kliewer, S., Willson, T. M. & Edwards, P. A., Jan 25 2002, In : Journal of Biological Chemistry. 277, 4, p. 2908-2915 8 p.

Research output: Contribution to journalArticle

718 Scopus citations

Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα

Xu, H. E., Stanley, T. B., Montana, V. G., Lambert, M. H., Shearer, B. G., Cobb, J. E., McKee, D. D., Galardi, C. M., Plunket, K. D., Nolte, R. T., Parks, D. J., Moore, J. T., Kliewer, S. A., Willson, T. M. & Stimmel, J. B., Feb 14 2002, In : Nature. 415, 6873, p. 813-817 5 p.

Research output: Contribution to journalArticle

462 Scopus citations

The nuclear pregnane X receptor: A key regulator of xenobiotic metabolism

Kliewer, S. A., Goodwin, B. & Willson, T. M., Oct 1 2002, In : Endocrine reviews. 23, 5, p. 687-702 16 p.

Research output: Contribution to journalArticle

632 Scopus citations

Use of in vitro pregnane X receptor assays to assess CYP3A4 induction potential of drug candidates

Jones, S. A., Moore, L. B., Wisely, G. B. & Kliewer, S. A., Jan 1 2002, In : Methods in Enzymology. 357, p. 161-170 10 p.

Research output: Contribution to journalArticle

18 Scopus citations
2001

Adipose Tissue Resistin Expression is Severely Suppressed in Obesity and Stimulated by Peroxisome Proliferator-activated Receptor γ Agonists

Way, J. M., Görgün, C. Z., Tong, Q., Uysal, K. T., Brown, K. K., Harrington, W. W., Oliver, W. R., Willson, T. M., Kliewer, S. A. & Hotamisligil, G. S., Jul 13 2001, In : Journal of Biological Chemistry. 276, 28, p. 25651-25653 3 p.

Research output: Contribution to journalArticle

393 Scopus citations

A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport

Oliver, W. R., Shenk, J. L., Snaith, M. R., Russell, C. S., Plunket, K. D., Bodkin, N. L., Lewis, M. C., Winegar, D. A., Sznaidman, M. L., Lambert, M. H., Xu, H. E., Sternbach, D. D., Kliewer, S. A., Hansen, B. C. & Willson, T. M., Apr 24 2001, In : Proceedings of the National Academy of Sciences of the United States of America. 98, 9, p. 5306-5311 6 p.

Research output: Contribution to journalArticle

908 Scopus citations

Chemical genomics: Functional analysis of orphan nuclear receptors in the regulation of bile acid metabolism

Willson, T. M., Jones, S. A., Moore, J. T. & Kliewer, S. A., 2001, In : Medicinal Research Reviews. 21, 6, p. 513-522 10 p.

Research output: Contribution to journalArticle

99 Scopus citations

Comprehensive messenger ribonucleic acid profiling reveals that peroxisome proliferator-activated receptor γ activation has coordinate effects on gene expression in multiple insulin-sensitive tissues

Way, J. M., Harrington, W. W., Brown, K. K., Gottschalk, W. K., Sundseth, S. S., Mansfield, T. A., Ramachandran, R. K., Willson, T. M. & Kliewer, S. A., 2001, In : Endocrinology. 142, 3, p. 1269-1277 9 p.

Research output: Contribution to journalArticle

Open Access
295 Scopus citations

Effects of fenofibrate on lipid parameters in obese rhesus monkeys

Winegar, D. A., Brown, P. J., Wilkison, W. O., Lewis, M. C., Ott, R. J., Tong, W. Q., Brown, H. R., Lehmann, J. M., Kliewer, S. A., Plunket, K. D., Way, J. M., Bodkin, N. L. & Hansen, B. C., Nov 12 2001, In : Journal of lipid research. 42, 10, p. 1543-1551 9 p.

Research output: Contribution to journalArticle

63 Scopus citations

Liver X Receptor (LXR) Regulation of the LXRα Gene in Human Macrophages

Whitney, K. D., Watson, M. A., Goodwin, B., Galardi, C. M., Maglich, J. M., Wilson, J. G., Willson, T. M., Collins, J. L. & Kliewer, S. A., Nov 23 2001, In : Journal of Biological Chemistry. 276, 47, p. 43509-43515 7 p.

Research output: Contribution to journalArticle

132 Scopus citations

Regulation of the human CYP2B6 gene by the nuclear pregnane X receptor

Goodwin, B., Moore, L. B., Stoltz, C. M., McKee, D. D. & Kliewer, S. A., Sep 4 2001, In : Molecular Pharmacology. 60, 3, p. 427-431 5 p.

Research output: Contribution to journalArticle

344 Scopus citations

Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors

Xu, H. E., Lambert, M. H., Montana, V. G., Plunket, K. D., Moore, L. B., Collins, J. L., Oplinger, J. A., Kliewer, S. A., Gampe R.T., J., McKee, D. D., Moore, J. T. & Willson, T. M., Nov 20 2001, In : Proceedings of the National Academy of Sciences of the United States of America. 98, 24, p. 13919-13924 6 p.

Research output: Contribution to journalArticle

423 Scopus citations

The human nuclear xenobiotic receptor PXR: Structural determinants of directed promiscuity

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., Jun 22 2001, In : Science. 292, 5525, p. 2329-2333 5 p.

Research output: Contribution to journalArticle

659 Scopus citations

The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity

Staudinger, J. L., Goodwin, B., Jones, S. A., Hawkins-Brown, D., MacKenzie, K. I., LaTour, A., Liu, Y., Klaassen, C. D., Brown, K. K., Reinhard, J., Willson, T. M., Koller, B. H. & Kliewer, S. A., Mar 13 2001, In : Proceedings of the National Academy of Sciences of the United States of America. 98, 6, p. 3369-3374 6 p.

Research output: Contribution to journalArticle

1007 Scopus citations
2000

Alteration of a single amino acid in peroxisome proliferator-activated receptor-α (PPARα) generates a PPARδ phenotype

Takada, I., Yu, R. T., Xu, H. E., Lambert, M. H., Montana, V. G., Kliewer, S. A., Evans, R. M. & Umesono, K., Dec 1 2000, In : Molecular Endocrinology. 14, 5, p. 733-740 8 p.

Research output: Contribution to journalArticle

68 Scopus citations