TABLE 1

Possible models for inhibition of CYP2E1

ModelComplexes FormedBinding Allostery?Parameters and Consequencesa
Substrate (on Inhibitor)Inhibitor (on Substrate)
CompetitiveES, ESS, EINoNoKs, Kss, Ki, kcat
UncompetitiveES, ESS, ESINoNoKs, Kss, Ksi, kcat1, kcat2?
Mixed
Allosteric bothES, ESS, EI, ESIYesYesKs, Kss, Ki, Ksi, Kis, kcat1, kcat2?
Allosteric SubstrateES, ESS, EI, ESIYesNoKs, Kss, Ki, Ksi, Kis = Ks, kcat1, kcat2?
Allosteric inhibitorES, ESS, EI, ESINoYesKs, Kss, Ki = Ksi, Kis, kcat1, kcat2?
NoncompetitiveES, ESS, EI, ESINoNoKs, Kss, Ki = Ksi, Kis = Ks, kcat1, kcat2?
  • EI, enzyme-inhibitor.

  • a In all models except competitive, ESI may be active or not. Both possibilities were included in discriminations.