Examples of nonhyperbolic rate-substrate concentration profiles for CYP substrates using microsomal preparations of human liver and heterologously expressed systems
| Sigmoidal curves |
|---|
| Aflatoxin (Ueng et al., 1997 in E. coli and RFP) |
| Amitriptyline1-a (Schmider et al., 1995 in HLM; Shaw et al., 1997 in HLM and RFP; Ueng et al., 1997 in E. coli) |
| Carbamazepine1-b (Kerr et al., 1994 in HLM and VV;Korzekwa et al., 1998 in VV), |
| Desmethyladinazolam (Venkatakrishnan et al., 1998 in BV) |
| Diazepam1-b (Andersson et al., 1994 in HLM; Kenworthy et al., 1999b in β-LM; Shou et al., 1999 in BV) |
| Estradiol (Kerlan et al., 1992 in HLM; Ueng et al., 1997 in β-LM) |
| Nifedipine1-c (Shaw et al., 1997 in RFP and BV) |
| Nordiazepam (D. Carlile, N. Randolph, M. Bayliss and J.B.H., submitted in HLM and β-LM) |
| Progesterone1-d (Ueng et al., 1997 in β-LM; Domanski et al., 1998 in E. coli) |
| Testosterone1-e (Lee et al., 1995 in HLM and BV; Shaw et al., 1997 in HLM and BV; Ueng et al., 1997 in E. coli) |
| Convex curves |
| Midazolam1-f (Kronbach et al., 1989 in HLM; Ghosal et al., 1996 in HLM and β-LM) |
| Nifedipine1-c(Kenworthy et al., 1999b in β-LM) |
| Terfenadine1-g (Kenworthy et al., 1999b in β-LM) |
↵1-a Not seen in BV by Shaw et al., 1997.
↵1-b Not seen in E. coli by Ueng et al., 1997.
↵1-c Both sigmoidicity and convex curves reported for this substrate.
↵1-d Not seen in BV by Yamazaki and Shimada, 1997.
↵1-e Not seen in RFP by Shaw et al., 1997.
↵1-f Not seen in β-LM by Gorski et al., 1994.
↵1-g Not seen in RFP by Rodrigues et al., 1995.
HLM, human liver microsomes; VV, vaccinia virus; BV, baculovirus; RFP, recombinant fusion protein.