-
1
-
-
2442700486
-
Drug–drug, drug–dietary supplement, and drug–citrus fruit and other food interactions: What have we learned?
-
Huang SM, Lesko LJ (2004) Drug–drug, drug–dietary supplement, and drug–citrus fruit and other food interactions: what have we learned? J Clin Pharmacol 44:559–569
-
(2004)
J Clin Pharmacol
, vol.44
, pp. 559-569
-
-
Huang, S.M.1
Lesko, L.J.2
-
2
-
-
44049087422
-
New era in drug interaction evaluation: US Food and Drug Administration update on CYP enzymes, transporters, and the guidance process
-
Huang SM, Strong JM, Zhang L et al (2008) New era in drug interaction evaluation: US Food and Drug Administration update on CYP enzymes, transporters, and the guidance process. J Clin Pharmacol 48:662–670
-
(2008)
J Clin Pharmacol
, vol.48
, pp. 662-670
-
-
Huang, S.M.1
Strong, J.M.2
Zhang, L.3
-
3
-
-
0033864694
-
Pharmacokinetic interactions between sildenafil and saquinavir/ritonavir
-
Muirhead GJ, Wulff MB, Fielding A et al (2000) Pharmacokinetic interactions between sildenafil and saquinavir/ritonavir. Br J Clin Pharmacol 50:99–107
-
(2000)
Br J Clin Pharmacol
, vol.50
, pp. 99-107
-
-
Muirhead, G.J.1
Wulff, M.B.2
Fielding, A.3
-
4
-
-
77954943905
-
Metabolism of ramelteon in human liver microsomes and correlation with the effect of fluvoxamine on ramelteon pharmacokinetics
-
Obach RS, Ryder TF (2010) Metabolism of ramelteon in human liver microsomes and correlation with the effect of fluvoxamine on ramelteon pharmacokinetics. Drug Metab Dispos 38:1381–1391
-
(2010)
Drug Metab Dispos
, vol.38
, pp. 1381-1391
-
-
Obach, R.S.1
Ryder, T.F.2
-
5
-
-
0030068752
-
Rifampin drastically reduces plasma concentrations and effects of oral midazolam
-
Backman JT, Olkkola KT, Neuvonen PJ (1996) Rifampin drastically reduces plasma concentrations and effects of oral midazolam. Clin Pharmacol Ther 59:7–13
-
(1996)
Clin Pharmacol Ther
, vol.59
, pp. 7-13
-
-
Backman, J.T.1
Olkkola, K.T.2
Neuvonen, P.J.3
-
6
-
-
0030030330
-
Concentrations and effects of oral midazolam are greatly reduced in patients treated with carbamazepine or phenytoin
-
Backman JT, Olkkola KT, Ojala M et al (1996) Concentrations and effects of oral midazolam are greatly reduced in patients treated with carbamazepine or phenytoin. Epilepsia 37:253–257
-
(1996)
Epilepsia
, vol.37
, pp. 253-257
-
-
Backman, J.T.1
Olkkola, K.T.2
Ojala, M.3
-
7
-
-
33645837653
-
Duration of pleconaril effect on cytochrome P450 3A activity in healthy adults using the oral biomarker midazolam
-
Ma JD, Nafziger AN, Rhodes G et al (2006) Duration of pleconaril effect on cytochrome P450 3A activity in healthy adults using the oral biomarker midazolam. Drug Metab Dispos 34:783–785
-
(2006)
Drug Metab Dispos
, vol.34
, pp. 783-785
-
-
Ma, J.D.1
Nafziger, A.N.2
Rhodes, G.3
-
9
-
-
73349087148
-
Activation of pregnane X receptor (PXR) and constitutive androstane receptor (CAR) by herbal medicines
-
Chang TK (2009) Activation of pregnane X receptor (PXR) and constitutive androstane receptor (CAR) by herbal medicines. AAPS J 11:590–601
-
(2009)
AAPS J
, vol.11
, pp. 590-601
-
-
Chang, T.K.1
-
10
-
-
84872734709
-
Isoform-specific regulation of cytochromes p450 expression by estradiol and progesterone
-
Choi SY, Koh KH, Jeong H (2013) Isoform-specific regulation of cytochromes p450 expression by estradiol and progesterone. Drug Metab Dispos 41:263–269
-
(2013)
Drug Metab Dispos
, vol.41
, pp. 263-269
-
-
Choi, S.Y.1
Koh, K.H.2
Jeong, H.3
-
11
-
-
37549060373
-
Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination
-
Jeong H, Choi S, Song JW et al (2008) Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination. Xenobiotica 38:62–75
-
(2008)
Xenobiotica
, vol.38
, pp. 62-75
-
-
Jeong, H.1
Choi, S.2
Song, J.W.3
-
12
-
-
0018838326
-
Autoinduction of carbamazepine metabolism in children examined by a stable isotope technique
-
Bertilsson L, Hojer B, Tybring G et al (1980) Autoinduction of carbamazepine metabolism in children examined by a stable isotope technique. Clin Pharmacol Ther 27:83–88
-
(1980)
Clin Pharmacol Ther
, vol.27
, pp. 83-88
-
-
Bertilsson, L.1
Hojer, B.2
Tybring, G.3
-
13
-
-
0038434501
-
Artemisinin autoinduction is caused by involvement of cytochrome P450 2B6 but not 2C9
-
Simonsson US, Jansson B, Hai TN et al (2003) Artemisinin autoinduction is caused by involvement of cytochrome P450 2B6 but not 2C9. Clin Pharmacol Ther 74:32–43
-
(2003)
Clin Pharmacol Ther
, vol.74
, pp. 32-43
-
-
Simonsson, U.S.1
Jansson, B.2
Hai, T.N.3
-
14
-
-
0002485410
-
Pharmacokinetics: The dynamics of drug absorption, distribution, and elimination
-
Hardman J, Limbird L, Goodman Gilman A, 10th edn. McGraw-Hill, New York
-
Wilkinson GR (2001) Pharmacokinetics: the dynamics of drug absorption, distribution, and elimination. In: Hardman J, Limbird L, Goodman Gilman A (eds) The pharmacological basis of therapeutics, 10th edn. McGraw-Hill, New York
-
(2001)
The Pharmacological Basis of Therapeutics
-
-
Wilkinson, G.R.1
-
15
-
-
79955690629
-
-
Ema, Guideline on the investigation of drug interactions [Online]. , Accessed September 2012
-
Ema (2012) Guideline on the investigation of drug interactions. Guideline on the investigation of drug interactions [Online]. http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2012/07/WC500129606.pdf Accessed September 2012
-
(2012)
Guideline on the Investigation of Drug Interactions
-
-
-
16
-
-
84865415281
-
-
FDA, Guidance for industry: drug interaction studies-study design, data analysis, implications for dosing, and labeling recommendations [Online]
-
FDA (2012) Guidance for industry: drug interaction studies-study design, data analysis, implications for dosing, and labeling recommendations. Guidance for industry: drug interaction studies-study design, data analysis, implications for dosing, and labeling recommendations [Online]. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/ Guidances/UCM292362.pdf
-
(2012)
Guidance for Industry: Drug Interaction Studies-Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations
-
-
-
17
-
-
84863735141
-
Modulation of cytochrome-P450 inhibition (CYP) in drug discovery: A medicinal chemistry perspective
-
Kumar S, Sharma R, Roychowdhury A (2012) Modulation of cytochrome-P450 inhibition (CYP) in drug discovery: a medicinal chemistry perspective. Curr Med Chem 19:3605–3621
-
(2012)
Curr Med Chem
, vol.19
, pp. 3605-3621
-
-
Kumar, S.1
Sharma, R.2
Roychowdhury, A.3
-
18
-
-
0035659943
-
Dual effect of dexamethasone on CYP3A4 gene expression in human hepatocytes. Sequential role of glucocorticoid receptor and pregnane X receptor
-
Pascussi JM, Drocourt L, Gerbal-Chaloin S et al (2001) Dual effect of dexamethasone on CYP3A4 gene expression in human hepatocytes. Sequential role of glucocorticoid receptor and pregnane X receptor. Eur J Biochem 268:6346–6358
-
(2001)
Eur J Biochem
, vol.268
, pp. 6346-6358
-
-
Pascussi, J.M.1
Drocourt, L.2
Gerbal-Chaloin, S.3
-
19
-
-
84863122056
-
An insulin-like growth factor 1 receptor inhibitor induces CYP3A4 expression through a pregnane X receptor-independent, noncanonical constitutive androstane receptor-related mechanism
-
Li L, Sinz MW, Zimmermann K et al (2012) An insulin-like growth factor 1 receptor inhibitor induces CYP3A4 expression through a pregnane X receptor-independent, noncanonical constitutive androstane receptor-related mechanism. J Pharmacol Exp Ther 340:688–697
-
(2012)
J Pharmacol Exp Ther
, vol.340
, pp. 688-697
-
-
Li, L.1
Sinz, M.W.2
Zimmermann, K.3
-
20
-
-
33845953191
-
The 2006 Bernard B. Brodie Award Lecture. Cyp2e1
-
Gonzalez FJ (2007) The 2006 Bernard B. Brodie Award Lecture. Cyp2e1. Drug Metab Dispos 35:1–8
-
(2007)
Drug Metab Dispos
, vol.35
, pp. 1-8
-
-
Gonzalez, F.J.1
-
21
-
-
33847024555
-
CAR and PXR: The xenobiotic-sensing receptors
-
Timsit YE, Negishi M (2007) CAR and PXR: the xenobiotic-sensing receptors. Steroids 72:231–246
-
(2007)
Steroids
, vol.72
, pp. 231-246
-
-
Timsit, Y.E.1
Negishi, M.2
-
22
-
-
67651207389
-
Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening
-
Shukla SJ, Nguyen DT, Macarthur R et al (2009) Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening. Assay Drug Dev Technol 7:143–169
-
(2009)
Assay Drug Dev Technol
, vol.7
, pp. 143-169
-
-
Shukla, S.J.1
Nguyen, D.T.2
Macarthur, R.3
-
23
-
-
78650748330
-
Identification of clinically used drugs that activate pregnane X receptors
-
Shukla SJ, Sakamuru S, Huang R et al (2011) Identification of clinically used drugs that activate pregnane X receptors. Drug Metab Dispos 39:151–159
-
(2011)
Drug Metab Dispos
, vol.39
, pp. 151-159
-
-
Shukla, S.J.1
Sakamuru, S.2
Huang, R.3
-
24
-
-
33646517938
-
Evaluation of 170 xenobiotics as transactivators of human pregnane X receptor (hPXR) and correlation to known CYP3A4 drug interactions
-
Sinz M, Kim S, Zhu Z et al (2006) Evaluation of 170 xenobiotics as transactivators of human pregnane X receptor (hPXR) and correlation to known CYP3A4 drug interactions. Curr Drug Metab 7:375–388
-
(2006)
Curr Drug Metab
, vol.7
, pp. 375-388
-
-
Sinz, M.1
Kim, S.2
Zhu, Z.3
-
25
-
-
69749083669
-
Nuclear receptors CAR and PXR: Molecular, functional, and biomedical aspects
-
Di Masi A, De Marinis E, Ascenzi P et al (2009) Nuclear receptors CAR and PXR: molecular, functional, and biomedical aspects. Mol Aspects Med 30:297–343
-
(2009)
Mol Aspects Med
, vol.30
, pp. 297-343
-
-
Di Masi, A.1
De Marinis, E.2
Ascenzi, P.3
-
26
-
-
33746924066
-
Ligand recognition by drug-activated nuclear receptors PXR and CAR: Structural, site-directed mutagenesis and molecular modeling studies
-
Poso A, Honkakoski P (2006) Ligand recognition by drug-activated nuclear receptors PXR and CAR: structural, site-directed mutagenesis and molecular modeling studies. Mini Rev Med Chem 6:937–947
-
(2006)
Mini Rev Med Chem
, vol.6
, pp. 937-947
-
-
Poso, A.1
Honkakoski, P.2
-
27
-
-
17744375160
-
The pregnane X receptor: A promiscuous xenobiotic receptor that has diverged during evolution
-
Jones SA, Moore LB, Shenk JL et al (2000) The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. Mol Endocrinol 14:27–39
-
(2000)
Mol Endocrinol
, vol.14
, pp. 27-39
-
-
Jones, S.A.1
Moore, L.B.2
Shenk, J.L.3
-
28
-
-
73149087257
-
Evaluation of cynomolgus monkey pregnane X receptor, primary hepatocyte, and in vivo pharmacokinetic changes in predicting human CYP3A4 induction
-
Kim S, Dinchuk JE, Anthony MN et al (2010) Evaluation of cynomolgus monkey pregnane X receptor, primary hepatocyte, and in vivo pharmacokinetic changes in predicting human CYP3A4 induction. Drug Metab Dispos 38:16–24
-
(2010)
Drug Metab Dispos
, vol.38
, pp. 16-24
-
-
Kim, S.1
Dinchuk, J.E.2
Anthony, M.N.3
-
29
-
-
0036799870
-
The nuclear pregnane X receptor: A key regulator of xenobiotic metabolism
-
Kliewer SA, Goodwin B, Willson TM (2002) The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism. Endocr Rev 23:687–702
-
(2002)
Endocr Rev
, vol.23
, pp. 687-702
-
-
Kliewer, S.A.1
Goodwin, B.2
Willson, T.M.3
-
30
-
-
34548532926
-
Comparison of inducibility of CYP1A and CYP3A mRNAs by prototypical inducers in primary cultures of human, cynomolgus monkey, and rat hepatocytes
-
Nishimura M, Koeda A, Suganuma Y et al (2007) Comparison of inducibility of CYP1A and CYP3A mRNAs by prototypical inducers in primary cultures of human, cynomolgus monkey, and rat hepatocytes. Drug Metab Pharmacokinet 22:178–186
-
(2007)
Drug Metab Pharmacokinet
, vol.22
, pp. 178-186
-
-
Nishimura, M.1
Koeda, A.2
Suganuma, Y.3
-
31
-
-
33747868126
-
In vitro and in vivo CYP3A64 induction and inhibition studies in rhesus monkeys: A preclinical approach for CYP3A-mediated drug interaction studies
-
Prueksaritanont T, Kuo Y, Tang C et al (2006) In vitro and in vivo CYP3A64 induction and inhibition studies in rhesus monkeys: a preclinical approach for CYP3A-mediated drug interaction studies. Drug Metab Dispos 34:1546–1555
-
(2006)
Drug Metab Dispos
, vol.34
, pp. 1546-1555
-
-
Prueksaritanont, T.1
Kuo, Y.2
Tang, C.3
-
32
-
-
23144467497
-
Structure and function of the human nuclear xenobiotic receptor PXR
-
Carnahan VE, Redinbo MR (2005) Structure and function of the human nuclear xenobiotic receptor PXR. Curr Drug Metab 6:357–367
-
(2005)
Curr Drug Metab
, vol.6
, pp. 357-367
-
-
Carnahan, V.E.1
Redinbo, M.R.2
-
33
-
-
50449111314
-
Nuclear receptor drug discovery
-
Chen T (2008) Nuclear receptor drug discovery. Curr Opin Chem Biol 12:418–426
-
(2008)
Curr Opin Chem Biol
, vol.12
, pp. 418-426
-
-
Chen, T.1
-
34
-
-
77956234759
-
Camptothecin attenuates cytochrome P450. 3A4 induction by blocking the activation of human pregnane X receptor
-
Chen Y, Tang Y, Robbins GT et al (2010) Camptothecin attenuates cytochrome P450. 3A4 induction by blocking the activation of human pregnane X receptor. J Pharmacol Exp Ther 334:999–1008
-
(2010)
J Pharmacol Exp Ther
, vol.334
, pp. 999-1008
-
-
Chen, Y.1
Tang, Y.2
Robbins, G.T.3
-
35
-
-
33846230463
-
Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole
-
Huang H, Wang H, Sinz M et al (2007) Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole. Oncogene 26:258–268
-
(2007)
Oncogene
, vol.26
, pp. 258-268
-
-
Huang, H.1
Wang, H.2
Sinz, M.3
-
36
-
-
84862275724
-
Sesamin: A naturally occurring lignan inhibits CYP3A4 by antagonizing the pregnane X receptor activation
-
Lim YP, Ma CY, Liu CL et al (2012) Sesamin: a naturally occurring lignan inhibits CYP3A4 by antagonizing the pregnane X receptor activation. Evid Based Complement Alternat Med 2012:242810
-
(2012)
Evid Based Complement Alternat Med
, vol.2012
-
-
Lim, Y.P.1
Ma, C.Y.2
Liu, C.L.3
-
37
-
-
66649089506
-
Evaluation of multiple in vitro systems for assessment of CYP3A4 induction in drug discovery: Human hepatocytes, pregnane X receptor reporter gene, and Fa2N-4 and HepaRG cells
-
Mcginnity DF, Zhang G, Kenny JR et al (2009) Evaluation of multiple in vitro systems for assessment of CYP3A4 induction in drug discovery: human hepatocytes, pregnane X receptor reporter gene, and Fa2N-4 and HepaRG cells. Drug Metab Dispos 37:1259–1268
-
(2009)
Drug Metab Dispos
, vol.37
, pp. 1259-1268
-
-
McGinnity, D.F.1
Zhang, G.2
Kenny, J.R.3
-
38
-
-
79851505734
-
Current in vitro high throughput screening approaches to assess nuclear receptor activation
-
Raucy JL, Lasker JM (2010) Current in vitro high throughput screening approaches to assess nuclear receptor activation. Curr Drug Metab 11:806–814
-
(2010)
Curr Drug Metab
, vol.11
, pp. 806-814
-
-
Raucy, J.L.1
Lasker, J.M.2
-
39
-
-
53849093733
-
Current industrial practices in assessing CYP450 enzyme induction: Preclinical and clinical
-
Sinz M, Wallace G, Sahi J (2008) Current industrial practices in assessing CYP450 enzyme induction: preclinical and clinical. AAPS J 10:391–400
-
(2008)
AAPS J
, vol.10
, pp. 391-400
-
-
Sinz, M.1
Wallace, G.2
Sahi, J.3
-
40
-
-
16644388319
-
Correlation of high-throughput pregnane X receptor (PXR) transactivation and binding assays
-
Zhu Z, Kim S, Chen T et al (2004) Correlation of high-throughput pregnane X receptor (PXR) transactivation and binding assays. J Biomol Screen 9:533–540
-
(2004)
J Biomol Screen
, vol.9
, pp. 533-540
-
-
Zhu, Z.1
Kim, S.2
Chen, T.3
-
41
-
-
33847614798
-
Use of cryopreserved transiently transfected cells in high-throughput pregnane X receptor transactivation assay
-
Zhu Z, Puglisi J, Connors D et al (2007) Use of cryopreserved transiently transfected cells in high-throughput pregnane X receptor transactivation assay. J Biomol Screen 12:248–254
-
(2007)
J Biomol Screen
, vol.12
, pp. 248-254
-
-
Zhu, Z.1
Puglisi, J.2
Connors, D.3
-
42
-
-
49149108728
-
Application and interpretation of hPXR screening data: Validation of reporter signal requirements for prediction of clinically relevant CYP3A4 inducers
-
Cui X, Thomas A, Gerlach V et al (2008) Application and interpretation of hPXR screening data: Validation of reporter signal requirements for prediction of clinically relevant CYP3A4 inducers. Biochem Pharmacol 76:680–689
-
(2008)
Biochem Pharmacol
, vol.76
, pp. 680-689
-
-
Cui, X.1
Thomas, A.2
Gerlach, V.3
-
43
-
-
0034781795
-
Use of a reporter gene assay to predict and rank the potency and efficacy of CYP3A4 inducers
-
El-Sankary W, Gibson GG, Ayrton A et al (2001) Use of a reporter gene assay to predict and rank the potency and efficacy of CYP3A4 inducers. Drug Metab Dispos 29:1499–1504
-
(2001)
Drug Metab Dispos
, vol.29
, pp. 1499-1504
-
-
El-Sankary, W.1
Gibson, G.G.2
Ayrton, A.3
-
44
-
-
67649404709
-
In vitro and in vivo induction of cytochrome p450: A survey of the current practices and recommendations: A pharmaceutical research and manufacturers of America perspective
-
Chu V, Einolf HJ, Evers R et al (2009) In vitro and in vivo induction of cytochrome p450: a survey of the current practices and recommendations: a pharmaceutical research and manufacturers of America perspective. Drug Metab Dispos 37:1339–1354
-
(2009)
Drug Metab Dispos
, vol.37
, pp. 1339-1354
-
-
Chu, V.1
Einolf, H.J.2
Evers, R.3
-
45
-
-
77958498196
-
Evaluation of models for predicting drug–drug interactions due to induction
-
Fahmi OA, Ripp SL (2010) Evaluation of models for predicting drug–drug interactions due to induction. Expert Opin Drug Metab Toxicol 6:1399–1416
-
(2010)
Expert Opin Drug Metab Toxicol
, vol.6
, pp. 1399-1416
-
-
Fahmi, O.A.1
Ripp, S.L.2
-
46
-
-
34247505094
-
Induction of drug metabolizing enzymes: A survey of in vitro methodologies and interpretations used in the pharmaceutical industry–do they comply with FDA recommendations?
-
Hewitt NJ, De Kanter R, Lecluyse E (2007) Induction of drug metabolizing enzymes: a survey of in vitro methodologies and interpretations used in the pharmaceutical industry–do they comply with FDA recommendations? Chem Biol Interact 168:51–65
-
(2007)
Chem Biol Interact
, vol.168
, pp. 51-65
-
-
Hewitt, N.J.1
De Kanter, R.2
Lecluyse, E.3
-
47
-
-
33645972546
-
Stem cells, immortalized cells, and primary cells in ADMET assays
-
Sinz M, Kim S (2006) Stem cells, immortalized cells, and primary cells in ADMET assays. Drug Discov Today Technol 3:79–85
-
(2006)
Drug Discov Today Technol
, vol.3
, pp. 79-85
-
-
Sinz, M.1
Kim, S.2
-
48
-
-
80052011288
-
Quantitative prediction of human pregnane X receptor and cytochrome P450 3A4 mediated drug-drug interaction in a novel multiple humanized mouse line
-
Hasegawa M, Kapelyukh Y, Tahara H et al (2011) Quantitative prediction of human pregnane X receptor and cytochrome P450 3A4 mediated drug-drug interaction in a novel multiple humanized mouse line. Mol Pharmacol 80:518–528
-
(2011)
Mol Pharmacol
, vol.80
, pp. 518-528
-
-
Hasegawa, M.1
Kapelyukh, Y.2
Tahara, H.3
-
49
-
-
53749106271
-
Quantitative relationship between rifampicin exposure and induction of Cyp3a11 in SXR humanized mice: Extrapolation to human CYP3A4 induction potential
-
Kim S, Pray D, Zheng M et al (2008) Quantitative relationship between rifampicin exposure and induction of Cyp3a11 in SXR humanized mice: extrapolation to human CYP3A4 induction potential. Drug Metab Lett 2:169–175
-
(2008)
Drug Metab Lett
, vol.2
, pp. 169-175
-
-
Kim, S.1
Pray, D.2
Zheng, M.3
-
50
-
-
33847056693
-
Attenuating pregnane X receptor (PXR) activation: A molecular modelling approach
-
Gao YD, Olson SH, Balkovec JM et al (2007) Attenuating pregnane X receptor (PXR) activation: a molecular modelling approach. Xenobiotica 37:124–138
-
(2007)
Xenobiotica
, vol.37
, pp. 124-138
-
-
Gao, Y.D.1
Olson, S.H.2
Balkovec, J.M.3
-
51
-
-
18444374978
-
The identification of ligand features essential for PXR activation by pharmacophore modeling
-
Schuster D, Langer T (2005) The identification of ligand features essential for PXR activation by pharmacophore modeling. J Chem Inf Model 45:431–439
-
(2005)
J Chem Inf Model
, vol.45
, pp. 431-439
-
-
Schuster, D.1
Langer, T.2
-
52
-
-
77955654799
-
Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists
-
Schlegel KA, Yang ZQ, Reger TS et al (2010) Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists. Bioorg Med Chem Lett 20: 5147–5152
-
(2010)
Bioorg Med Chem Lett
, vol.20
, pp. 5147-5152
-
-
Schlegel, K.A.1
Yang, Z.Q.2
Reger, T.S.3
-
53
-
-
22244435560
-
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase
-
Harper S, Avolio S, Pacini B et al (2005) Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase. J Med Chem 48:4547–4557
-
(2005)
J Med Chem
, vol.48
, pp. 4547-4557
-
-
Harper, S.1
Avolio, S.2
Pacini, B.3
-
54
-
-
58149087619
-
Further studies with the 2-amino-1,3-thiazol- 4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: Reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model
-
Fotsch C, Bartberger MD, Bercot EA et al (2008) Further studies with the 2-amino-1,3-thiazol- 4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model. J Med Chem 51:7953–7967
-
(2008)
J Med Chem
, vol.51
, pp. 7953-7967
-
-
Fotsch, C.1
Bartberger, M.D.2
Bercot, E.A.3
-
55
-
-
61349172663
-
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors
-
Rew Y, Mcminn DL, Wang Z et al (2009) Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors. Bioorg Med Chem Lett 19:1797–1801
-
(2009)
Bioorg Med Chem Lett
, vol.19
, pp. 1797-1801
-
-
Rew, Y.1
McMinn, D.L.2
Wang, Z.3
-
56
-
-
77955422082
-
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines
-
Kaizerman JA, Aaron W, An S et al (2010) Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines. Bioorg Med Chem Lett 20: 4607–4610
-
(2010)
Bioorg Med Chem Lett
, vol.20
, pp. 4607-4610
-
-
Kaizerman, J.A.1
Aaron, W.2
An, S.3
-
57
-
-
76649090591
-
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors
-
Zimmermann K, Wittman MD, Saulnier MG et al (2010) SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. Bioorg Med Chem Lett 20:1744–1748
-
(2010)
Bioorg Med Chem Lett
, vol.20
, pp. 1744-1748
-
-
Zimmermann, K.1
Wittman, M.D.2
Saulnier, M.G.3
-
58
-
-
47949086965
-
Machine learning methods and docking for predicting human pregnane X receptor activation
-
Khandelwal A, Krasowski MD, Reschly EJ et al (2008) Machine learning methods and docking for predicting human pregnane X receptor activation. Chem Res Toxicol 21: 1457–1467
-
(2008)
Chem Res Toxicol
, vol.21
, pp. 1457-1467
-
-
Khandelwal, A.1
Krasowski, M.D.2
Reschly, E.J.3
-
59
-
-
34447133457
-
New opportunities for pregnane X receptor (PXR) targeting in drug development. Lessons from Enantio- and species-specific PXR ligands identified from a discovery library of amino acid analogues
-
Wipf P, Gong H, Janjic JM et al (2007) New opportunities for pregnane X receptor (PXR) targeting in drug development. lessons from Enantio- and species-specific PXR ligands identified from a discovery library of amino acid analogues. Mini Rev Med Chem 7:617–625
-
(2007)
Mini Rev Med Chem
, vol.7
, pp. 617-625
-
-
Wipf, P.1
Gong, H.2
Janjic, J.M.3
-
60
-
-
0346099111
-
Role of orphan nuclear receptors in the regulation of drugmetabolising enzymes
-
Wang H, Lecluyse EL (2003) Role of orphan nuclear receptors in the regulation of drugmetabolising enzymes. Clin Pharmacokinet 42:1331–1357
-
(2003)
Clin Pharmacokinet
, vol.42
, pp. 1331-1357
-
-
Wang, H.1
Lecluyse, E.L.2
-
61
-
-
84873433884
-
Identification of novel activators of constitutive androstane receptor from FDA-approved drugs by integrated computational and biological approaches
-
Lynch C, Pan Y, Li L et al (2012) Identification of novel activators of constitutive androstane receptor from FDA-approved drugs by integrated computational and biological approaches. Pharm Res 30:489–501
-
(2012)
Pharm Res
, vol.30
, pp. 489-501
-
-
Lynch, C.1
Pan, Y.2
Li, L.3
-
62
-
-
84916235542
-
Structure and function of PXR and CAR
-
XieW(ed) , Wiley, Hoboken
-
Zhou X, Xu H (2009) Structure and function of PXR and CAR. In: XieW(ed) Nuclear receptors in drug metabolism. Wiley, Hoboken
-
(2009)
Nuclear Receptors in Drug Metabolism
-
-
Zhou, X.1
Xu, H.2
-
63
-
-
19944372389
-
A structural basis for constitutive activity in the human CAR/RXRalpha heterodimer
-
Xu RX, Lambert MH, Wisely BB et al (2004) A structural basis for constitutive activity in the human CAR/RXRalpha heterodimer. Mol Cell 16:919–928
-
(2004)
Mol Cell
, vol.16
, pp. 919-928
-
-
Xu, R.X.1
Lambert, M.H.2
Wisely, B.B.3
-
64
-
-
80054732029
-
Constitutive androstane receptor (CAR) is a xenosensor and target for therapy
-
Kachaylo EM, Pustylnyak VO, Lyakhovich VV et al (2011) Constitutive androstane receptor (CAR) is a xenosensor and target for therapy. Biochemistry (Mosc) 76:1087–1097
-
(2011)
Biochemistry (Mosc)
, vol.76
, pp. 1087-1097
-
-
Kachaylo, E.M.1
Pustylnyak, V.O.2
Lyakhovich, V.V.3
-
65
-
-
79952625582
-
Modulation of constitutive androstane receptor (CAR) and pregnane X receptor (PXR) by 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives, ligands of peripheral benzodiazepine receptor (PBR)
-
Anderson LE, Dring AM, Hamel LD et al (2011) Modulation of constitutive androstane receptor (CAR) and pregnane X receptor (PXR) by 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives, ligands of peripheral benzodiazepine receptor (PBR). Toxicol Lett 202:148–154
-
(2011)
Toxicol Lett
, vol.202
, pp. 148-154
-
-
Anderson, L.E.1
Dring, A.M.2
Hamel, L.D.3
-
66
-
-
82955240628
-
New in vitro tools to study human constitutive androstane receptor (CAR) biology: Discovery and comparison of human CAR inverse agonists
-
Kublbeck J, Jyrkkarinne J, Molnar F et al (2011) New in vitro tools to study human constitutive androstane receptor (CAR) biology: discovery and comparison of human CAR inverse agonists. Mol Pharm 8:2424–2433
-
(2011)
Mol Pharm
, vol.8
, pp. 2424-2433
-
-
Kublbeck, J.1
Jyrkkarinne, J.2
Molnar, F.3
-
67
-
-
33845881481
-
Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers
-
Faucette SR, Zhang TC, Moore R et al (2007) Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. J Pharmacol Exp Ther 320:72–80
-
(2007)
J Pharmacol Exp Ther
, vol.320
, pp. 72-80
-
-
Faucette, S.R.1
Zhang, T.C.2
Moore, R.3
-
68
-
-
77956817177
-
A consecutive three alanine residue insertion mutant of human CAR: A novel CAR ligand screening system in HepG2 cells
-
Kanno Y, Inouye Y (2010) A consecutive three alanine residue insertion mutant of human CAR: a novel CAR ligand screening system in HepG2 cells. J Toxicol Sci 35:515–525
-
(2010)
J Toxicol Sci
, vol.35
, pp. 515-525
-
-
Kanno, Y.1
Inouye, Y.2
-
69
-
-
80555149413
-
Use of comprehensive screening methods to detect selective human CAR activators
-
Kublbeck J, Laitinen T, Jyrkkarinne J et al (2011) Use of comprehensive screening methods to detect selective human CAR activators. Biochem Pharmacol 82:1994–2007
-
(2011)
Biochem Pharmacol
, vol.82
, pp. 1994-2007
-
-
Kublbeck, J.1
Laitinen, T.2
Jyrkkarinne, J.3
-
70
-
-
41149153511
-
The tangle of nuclear receptors that controls xenobiotic metabolism and transport: Crosstalk and consequences
-
Pascussi JM, Gerbal-Chaloin S, Duret C et al (2008) The tangle of nuclear receptors that controls xenobiotic metabolism and transport: crosstalk and consequences. Annu Rev Pharmacol Toxicol 48:1–32
-
(2008)
Annu Rev Pharmacol Toxicol
, vol.48
, pp. 1-32
-
-
Pascussi, J.M.1
Gerbal-Chaloin, S.2
Duret, C.3
-
71
-
-
66449126809
-
Nuclear translocation of adenoviral-enhanced yellow fluorescent protein-tagged-human constitutive androstane receptor (hCAR): A novel tool for screening hCAR activators in human primary hepatocytes
-
Li H, Chen T, Cottrell J et al (2009) Nuclear translocation of adenoviral-enhanced yellow fluorescent protein-tagged-human constitutive androstane receptor (hCAR): a novel tool for screening hCAR activators in human primary hepatocytes. Drug Metab Dispos 37:1098–1106
-
(2009)
Drug Metab Dispos
, vol.37
, pp. 1098-1106
-
-
Li, H.1
Chen, T.2
Cottrell, J.3
-
72
-
-
84878862550
-
3D structure and ligand specificity of nuclear xenobiotic receptors CAR, PXR and VDR
-
Wu B, Li S, Dong D (2013) 3D structure and ligand specificity of nuclear xenobiotic receptors CAR, PXR and VDR. Drug Discov Today 18:574–581
-
(2013)
Drug Discov Today
, vol.18
, pp. 574-581
-
-
Wu, B.1
Li, S.2
Dong, D.3
-
73
-
-
79957647874
-
Effect of several analogs of 2,4,6- triphenyldioxane-1,3 on constitutive androstane receptor activation
-
Pustylnyak V, Yarushkin A, Kachaylo E et al (2011) Effect of several analogs of 2,4,6- triphenyldioxane-1,3 on constitutive androstane receptor activation. Chem Biol Interact 192: 177–183
-
(2011)
Chem Biol Interact
, vol.192
, pp. 177-183
-
-
Pustylnyak, V.1
Yarushkin, A.2
Kachaylo, E.3
-
74
-
-
56749173772
-
Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis
-
Repo S, Jyrkkarinne J, Pulkkinen JT et al (2008) Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. J Med Chem 51:7119–7131
-
(2008)
J Med Chem
, vol.51
, pp. 7119-7131
-
-
Repo, S.1
Jyrkkarinne, J.2
Pulkkinen, J.T.3
-
75
-
-
78149468556
-
Rational quantitative structure-activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands
-
Dring AM, Anderson LE, Qamar S et al (2010) Rational quantitative structure-activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands. Chem Biol Interact 188:512–525
-
(2010)
Chem Biol Interact
, vol.188
, pp. 512-525
-
-
Dring, A.M.1
Erson, L.E.2
Qamar, S.3
-
76
-
-
54049118742
-
Discovery of substituted sulfonamides and thiazolidin-4-one derivatives as agonists of human constitutive androstane receptor
-
Kublbeck J, Jyrkkarinne J, Poso A et al (2008) Discovery of substituted sulfonamides and thiazolidin-4-one derivatives as agonists of human constitutive androstane receptor. Biochem Pharmacol 76:1288–1297
-
(2008)
Biochem Pharmacol
, vol.76
, pp. 1288-1297
-
-
Kublbeck, J.1
Jyrkkarinne, J.2
Poso, A.3
-
77
-
-
56749177315
-
Insights into ligand-elicited activation of human constitutive androstane receptor based on novel agonists and three-dimensional quantitative structure-activity relationship
-
Jyrkkarinne J, Windshugel B, Ronkko T et al (2008) Insights into ligand-elicited activation of human constitutive androstane receptor based on novel agonists and three-dimensional quantitative structure-activity relationship. J Med Chem 51:7181–7192
-
(2008)
J Med Chem
, vol.51
, pp. 7181-7192
-
-
Jyrkkarinne, J.1
Windshugel, B.2
Ronkko, T.3
-
78
-
-
59149090185
-
Coordinate regulation of human drug-metabolizing enzymes, and conjugate transporters by the Ah receptor, pregnane X receptor and constitutive androstane receptor
-
Kohle C, Bock KW (2009) Coordinate regulation of human drug-metabolizing enzymes, and conjugate transporters by the Ah receptor, pregnane X receptor and constitutive androstane receptor. Biochem Pharmacol 77:689–699
-
(2009)
Biochem Pharmacol
, vol.77
, pp. 689-699
-
-
Kohle, C.1
Bock, K.W.2
-
79
-
-
77949911622
-
Activation of xenobiotic receptors: Driving into the nucleus
-
Li H, Wang H (2010) Activation of xenobiotic receptors: driving into the nucleus. Expert Opin Drug Metab Toxicol 6:409–426
-
(2010)
Expert Opin Drug Metab Toxicol
, vol.6
, pp. 409-426
-
-
Li, H.1
Wang, H.2
-
80
-
-
41549114526
-
Xenobiotic-induced transcriptional regulation of xenobiotic metabolizing enzymes of the cytochrome P450 superfamily in human extrahepatic tissues
-
Pavek P, Dvorak Z (2008) Xenobiotic-induced transcriptional regulation of xenobiotic metabolizing enzymes of the cytochrome P450 superfamily in human extrahepatic tissues. Curr Drug Metab 9:129–143
-
(2008)
Curr Drug Metab
, vol.9
, pp. 129-143
-
-
Pavek, P.1
Dvorak, Z.2
-
81
-
-
78650175257
-
Regulation of drug-metabolizing enzymes by xenobiotic receptors: PXR and CAR
-
Tolson AH, Wang H (2010) Regulation of drug-metabolizing enzymes by xenobiotic receptors: PXR and CAR. Adv Drug Deliv Rev 62:1238–1249
-
(2010)
Adv Drug Deliv Rev
, vol.62
, pp. 1238-1249
-
-
Tolson, A.H.1
Wang, H.2
|