Table 3

Substrates reported to display substrate inhibition kinetics in various in vitro systems

SubstratePathwayEnzyme SourceReference
BenzyloxyresorufinResorufin formationBaculovirus-expressed CYP3A4 Lin et al., 2001
CelecoxibHydroxylationBaculovirus-expressed CYP2C9 Lin et al., 2001
CelecoxibHydroxylationHLM Tang et al., 2000
Dextromethorphan O-DemethylationBaculovirus-expressed CYP2D6 Lin et al., 2001
EthoxyresorufinResorufin formationBaculovirus-expressed CYP1A2 Lin et al., 2001
FluoxetineDemethylationHLM Stevens and Wrighton, 1993
FluoxetineDemethylationHLM Ring et al., 2001
HalothaneTFA formation3-a cDNA-expressed CYP2E13-a Spracklin et al., 1997
HalothaneBromide formationcDNA-expressed CYP2E13-a Ibid.
Progesterone6β-HydroxylationBaculovirus-expressed CYP3A4 Lin et al., 2001
Tenoxicam5′-HydroxylationHLM Zhao et al., 1992
Testosterone6β-HydroxylationBaculovirus-expressed CYP3A4 Lin et al., 2001
Triazolam1′-HydroxylationHLM Schrag and Wienkers, 2001

  • HLM, human liver microsomes; TFA, trifluoroacetic acid.

  • ↵3-a  Obtained from GENTEST.