Examples of autoactivation kinetics (homotropic positive cooperativity)
| Substrate | Pathway | Enzyme Source | Reference |
|---|---|---|---|
| Dapsone | Hydroxylation | Vaccinia-expressed CYP2C9 | Korzekwa et al., 1998 |
| Diazepam | 3-Hydroxylation | Baculovirus-expressed CYP3A4 | Shou et al., 1999 |
| Diazepam | 3-Hydroxylation | B-Lymphoblastoid-expressed CYP3A4 | Kenworthy et al., 2001 |
| Diazepam | Demethylation | Baculovirus-expressed CYP3A4 | Shou et al., 1999 |
| Testosterone | 16β-Hydroxylation | B-Lymphoblastoid-expressed CYP2B62-a | Ekins et al., 1998b |
| Testosterone | 6β-Hydroxylation | B-Lymphoblastoid-expressed CYP3A4 | Kenworthy et al., 2001 |
| Acetaminophen | O-Glucuronidation | HLM | Fisher et al., 2000 |
| Estradiol | 3-Glucuronidation | HLM | Ibid. |
For a more comprehensive review, see Ekins et al. (1998a) orHouston and Kenworthy (2000).
HLM, human liver microsomes.
↵2-a Obtained from GENTEST.