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Mechanism-based inactivation of human liver cytochrome P450 2A6 by 8-methoxypsoralen.
TLDR
Potency and selectivity suggest that 8-MOP could be a useful tool in vitro for evaluating P450 2A6 activity in various enzyme preparations.
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Mechanism-based inactivation of cytochrome P450 2B1 by 8-methoxypsoralen and several other furanocoumarins.
TLDR
8-MOP was found to be the most potent inactivators of purified reconstituted cytochrome P450 (P450) 2B1, and was characterized by LC electrospray ionization tandem mass spectrometry (ESI-MS/MS) as dihydro diols.
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Mechanism-based inactivation of P450 2A6 by furanocoumarins.
TLDR
The results suggest that relative to the cell system, more reactive intermediates can escape, rather than bind to, the active site of purified reconstituted P450 2A6.
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Oxidation of acetaminophen to its toxic quinone imine and nontoxic catechol metabolites by baculovirus-expressed and purified human cytochromes P450 2E1 and 2A6.
TLDR
Although at toxic doses of APAP P 450 2E1 is the more efficient catalyst for the formation of the toxic metabolite NAPQI, P450 2A6 also can contribute significantly to NAPZI production.
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(R)-(+)-Menthofuran is a potent, mechanism-based inactivator of human liver cytochrome P450 2A6.
TLDR
Addition of various nucleophiles, a chelator of iron, or scavengers of reactive oxygen species or extensive dialysis failed to protect CYP2A6 from inactivation, and menthofuran caused a time- and concentration-dependent loss of CYP 2A6 activity.
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Metabolism of (R)-(+)-pulegone and (R)-(+)-menthofuran by human liver cytochrome P-450s: evidence for formation of a furan epoxide.
TLDR
Two P-450s were found to oxidize menthofuran to a newly identified metabolite, 2-hydroxymenthofuran, which is an intermediate in the formation of the known metabolites mintlactone and isomintlact one.
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Electrospray ionization mass spectrometric analysis of intact cytochrome P450: identification of tienilic acid adducts to P450 2C9.
TLDR
Application of this HPLC/ESI-MS technique made the detection of the covalent modification to P450 2C9 following mechanism-based inactivation by tienilic acid possible.
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( R )-( 1 )-MENTHOFURAN IS A POTENT , MECHANISM-BASED INACTIVATOR OF HUMAN LIVER CYTOCHROME P 450 2 A 6
TLDR
Menthofuran is a potent, mechanism-based inactivator of human liver cytochrome P450 (CYP or P450) 2A6 and appears to be the major proximate toxin, based on toxicokinetic studies.
MECHANISM-BASED INACTIVATION OF HUMAN LIVER CYTOCHROME P 450 2 A 6 BY 8-METHOXYPSORALEN
TLDR
Potency and selectivity suggest that 8MOP could be a useful tool in vitro for evaluating P450 2A6 activity in various enzyme preparations, and its variability has the potential of compromising quantitative assessment of its catalytic activity toward any particular compound.
Metabolism of (R)-(+)-pulegone and (R)-(+)-menthofuran by human liver microsomal cytochrome P450 enzymes
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