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Pregnane X receptor‐ and CYP3A4 ‐humanized mouse models and their applications
Author(s) -
Cheng Jie,
Ma Xiaochao,
Gonzalez Frank J
Publication year - 2011
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2010.01129.x
Subject(s) - pregnane x receptor , cyp3a4 , nuclear receptor , drug metabolism , pregnane , xenobiotic , constitutive androstane receptor , receptor , humanized mouse , pharmacology , biology , metabolism , chemistry , endocrinology , drug , biochemistry , in vivo , cytochrome p450 , enzyme , transcription factor , microbiology and biotechnology , genetics , gene
Pregnane X receptor (PXR) is a pivotal nuclear receptor modulating xenobiotic metabolism primarily through its regulation of CYP3A4, the most important enzyme involved in drug metabolism in humans. Due to the marked species differences in ligand recognition by PXR, PXR ‐humanized (hPXR) mice, and mice expressing human PXR and CYP3A4 (Tg3A4/hPXR) were established. hPXR and Tg3A4/hPXR mice are valuable models for investigating the role of PXR in xenobiotic metabolism and toxicity, in lipid, bile acid and steroid hormone homeostasis, and in the control of inflammation.