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  • Cholic Acid Feeding Leads to Increased CYP2D6 Expression in CYP2D6-Humanized Mice.

Cholic Acid Feeding Leads to Increased CYP2D6 Expression in CYP2D6-Humanized Mice.

Drug metabolism and disposition: the biological fate of chemicals (2017-02-06)
Xian Pan, Rebecca Kent, Kyoung-Jae Won, Hyunyoung Jeong
摘要

Cytochrome P450 2D6 (CYP2D6) is a major drug-metabolizing enzyme, but the factors governing transcriptional regulation of its expression remain poorly understood. Based on previous reports of small heterodimer partner (SHP) playing an important role as a transcriptional repressor of CYP2D6 expression, here we investigated how a known upstream regulator of SHP expression, namely cholestasis triggered by cholic acid (CA) feeding in mice, can lead to altered CYP2D6 expression. To this end, CYP2D6-humanized (Tg-

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1,7-二甲基黄嘌呤, ~98%, solid