Humanized PXR-CAR-CYP3A4/3A7 Mouse Publications

Humanized PXR-CAR-CYP3A4/3A7 Mouse Model Page

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Mejdrová I, et al.
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Mejdrová I, Dušek J, Škach K, Stefela A, Skoda J, Chalupský K, Dohnalová K, Pavkova I, Kronenberger T, Rashidian A, Smutná L, Duchoslav V, Smutny T, Pávek P, Nencka R
(2023) Discovery of Novel Human Constitutive Androstane Receptor Agonists with the Imidazo[1,2-a]pyridine Structure. J Med Chem 66(4):2422-2456
Skoda J, et al.
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Skoda J, Dohnalova K, Chalupsky K, Stahl A, Templin M, Maixnerova J, Micuda S, Grøntved L, Braeuning A, Pavek P
(2022) Off-target lipid metabolism disruption by the mouse constitutive androstane receptor ligand TCPOBOP in humanized mice. Biochem Pharmacol 197:114905
Ly JQ, et al.
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Ly JQ, Wong S, Liu L, Li R, Messick K, Chang JH
(2021) Investigating the Utility of Humanized Pregnane X Receptor-Constitutive Androstane Receptor-CYP3A4/7 Mouse Model to Assess CYP3A-Mediated Induction. Drug Metab Dispos 49(7):540-547
Skoda J, et al.
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Skoda J, Dusek J, Drastik M, Stefela A, Dohnalova K, Chalupsky K, Smutny T, Micuda S, Gerbal-Chaloin S, Pavek P
(2020) Diazepam Promotes Translocation of Human Constitutive Androstane Receptor (CAR) via Direct Interaction with the Ligand-Binding Domain. Cells 9(12)
Crosby M, et al.
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Crosby M, Riddick DS
(2019) Suppression of Hepatic CYP3A4 Expression and Activity by 3-Methylcholanthrene in Humanized PXR-CAR-CYP3A4/3A7 Mice. Drug Metab Dispos 47(3):279-282
Zhao Y, et al.
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Zhao Y, Lee MH, Paderu P, Lee A, Jimenez-Ortigosa C, Park S, Mansbach RS, Shaw KJ, Perlin DS
(2018) Significantly Improved Pharmacokinetics Enhances In Vivo Efficacy of APX001 against Echinocandin- and Multidrug-Resistant Candida Isolates in a Mouse Model of Invasive Candidiasis. Antimicrob Agents Chemother 62(10)
MacLeod AK, et al.
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MacLeod AK, Lin D, Huang JT, McLaughlin LA, Henderson CJ, Wolf CR
(2018) Identification of Novel Pathways of Osimertinib Disposition and Potential Implications for the Outcome of Lung Cancer Therapy. Clin Cancer Res 24(9):2138-2147
MacLeod AK, et al.
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MacLeod AK, McLaughlin LA, Henderson CJ, Wolf CR
(2015) Activation status of the pregnane X receptor influences vemurafenib availability in humanized mouse models. Cancer Res 75(21):4573-81
Choo EF, et al.
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Choo EF, Woolsey S, DeMent K, Ly J, Messick K, Qin A, Takahashi R
(2015) Use of transgenic mouse models to understand the oral disposition and drug-drug interaction potential of cobimetinib, a MEK inhibitor. Drug Metab Dispos 43(6):864-9
Ly JQ, et al.
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Ly JQ, Messick K, Qin A, Takahashi RH, Choo EF
(2017) Utility of CYP3A4 and PXR-CAR-CYP3A4/3A7 Transgenic Mouse Models To Assess the Magnitude of CYP3A4 Mediated Drug-Drug Interactions. Mol. Pharm. 14(5):1754-1759
Humanization
Tox & Safety Assessment
Scheer N, et al.
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Scheer N, Ross J, Rode A, Zevnik B, Niehaves S, Faust N, Wolf CR
(2008) A novel panel of mouse models to evaluate the role of human pregnane X receptor and constitutive androstane receptor in drug response. J. Clin. Invest. 118(9):3228-39
Scheer N, et al.
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Scheer N, Ross J, Kapelyukh Y, Rode A, Wolf CR
(2010) In vivo responses of the human and murine pregnane X receptor to dexamethasone in mice. Drug Metab. Dispos. 38(7):1046-53
Ross J, et al.
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Ross J, Plummer SM, Rode A, Scheer N, Bower CC, Vogel O, Henderson CJ, Wolf CR, Elcombe CR
(2010) Human constitutive androstane receptor (CAR) and pregnane X receptor (PXR) support the hypertrophic but not the hyperplastic response to the murine nongenotoxic hepatocarcinogens phenobarbital and chlordane in vivo. Toxicol. Sci. 116(2):452-66
Hasegawa M, et al.
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Hasegawa M, Kapelyukh Y, Tahara H, Seibler J, Rode A, Krueger S, Lee DN, Wolf CR, Scheer N
(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(3):518-28
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