Table 2

P450 3A4 mutants with altered steroid hydroxylase activity and/or response to flavonoid stimulation2-a

SRS3A4 MutantP450cam Residue EquivalentMetabolite Profileα-Naphthoflavone Stimulation
Testosterone
 2L210AT185AlteredAltered
 2L211AR186UnalteredAltered
 2L211FR186UnalteredAltered
 2D214E—2-b UnalteredAltered
 2L211F/D214ER186/—UnalteredAltered
Progesterone
 4F304AV247AlteredAltered
 4A305VG248AlteredAltered
 4T309AT252AlteredUnaltered
 5I369VL294AlteredAltered
 5A370VV295AlteredUnaltered
 5L373HD297AlteredAltered

  • ↵2-a The effector utilized in these assays was α-naphthoflavone at 25 μM.

  • ↵2-b There is no equivalent amino acid in an alignment of P450 3A4 with P450cam.