Downregulation of CYP1A2, CYP2B6, and CYP3A4 in Human Hepatocytes by Prolyl Hydroxylase Domain 2 Inhibitors via Hypoxia-Inducible Factor- α Stabilization

Hypoxia-inducible factor (HIF) is associated with the expression of CYP, but the underlying mechanism remains uncertain. In this study, we investigated the effect of HIF- stabilization caused by novel prolyl hydroxylase domain (PHD) 2 inhibitors, which are HIF- stabilizers that mimic hypoxia, on the...

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Veröffentlicht in:	Drug metabolism and disposition 2021-01, Vol.49 (1), p.20-30
Hauptverfasser:	Takano, Hiroki, Yamaguchi, Jun-Ichi, Kato, Sota, Hamada, Makoto, Tada, Mika, Endo, Hiromi
Format:	Artikel
Sprache:	eng
Schlagworte:	Constitutive Androstane Receptor - metabolism Cytochrome P-450 CYP1A2 - metabolism Cytochrome P-450 CYP2B6 - metabolism Cytochrome P-450 CYP3A - metabolism Down-Regulation Hepatocytes - drug effects Hepatocytes - metabolism Humans Hypoxia-Inducible Factor 1, alpha Subunit - metabolism Hypoxia-Inducible Factor-Proline Dioxygenases - antagonists & inhibitors Pregnane X Receptor - metabolism Prolyl-Hydroxylase Inhibitors - pharmacokinetics Protein Stability Retinoid X Receptors - metabolism
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