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• W2074887730 abstract "In vitro experiments were conducted to compare <i>k</i>_inact, <i>K</i>_I and inactivation efficiency (<i>k</i>_inact/<i>K</i>_I) of cytochrome P450 (P450) 2C9 by tienilic acid and (±)-suprofen using (<i>S</i>)-flurbiprofen, diclofenac, and (<i>S</i>)-warfarin as reporter substrates. Although the inactivation of P450 2C9 by tienilic acid when (<i>S</i>)-flurbiprofen and diclofenac were used as substrates was similar (efficiency of ∼9 ml/min/μmol), the inactivation kinetics were characterized by a sigmoidal profile. (±)-Suprofen inactivation of (<i>S</i>)-flurbiprofen and diclofenac hydroxylation was also described by a sigmoidal profile, although inactivation was markedly less efficient (∼1 ml/min/μmol). In contrast, inactivation of P450 2C9-mediated (<i>S</i>)-warfarin 7-hydroxylation by tienilic acid and (±)-suprofen was best fit to a hyperbolic equation, where inactivation efficiency was moderately higher (10 ml/min/μmol) and ∼3-fold higher (3 ml/min/μmol), respectively, relative to that of the other probe substrates, which argues for careful consideration of reporter substrate when mechanism-based inactivation of P450 2C9 is assessed in vitro. Further investigations into the increased inactivation seen with tienilic acid relative to that with (±)-suprofen revealed that tienilic acid is a higher affinity substrate with a spectral binding affinity constant (<i>K</i>_s) of 2 μM and an in vitro half-life of 5 min compared with a <i>K</i>_s of 21 μM and a 50 min in vitro half-life for (±)-suprofen. Lastly, a close analog of tienilic acid with the carboxylate functionality replaced by an oxirane ring was devoid of inactivation properties, which suggests that an ionic binding interaction with a positively charged residue in the P450 2C9 active site is critical for recognition and mechanism-based inactivation by these close structural analogs." @default.
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• W2074887730 date "2008-10-06" @default.
• W2074887730 modified "2023-10-14" @default.
• W2074887730 title "Mechanism-Based Inactivation of Cytochrome P450 2C9 by Tienilic Acid and (±)-Suprofen: A Comparison of Kinetics and Probe Substrate Selection" @default.
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• W2074887730 doi "https://doi.org/10.1124/dmd.108.023358" @default.
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