CYP1A2 |
CSM |
Region |
Function |
Reference |
E163K, K170Q |
6-7, 7 |
D helix |
Enhanced activity
Substrate selectivity |
25-28 |
V193M |
8-9 |
E helix |
E225N |
10 |
F helix |
|
Q258H |
11 |
G helix |
G437D |
18 |
K’-L loop |
CYP2A6 |
|
S183C |
7-8 |
E helix |
Enhanced activity
Altered substrate specificity
Novel activity |
29-32 |
L206Q, F209I |
8-9 |
F helix |
S224P |
9 |
F-G loop |
L240C |
10-11 |
G helix |
Y287H |
11-12 |
I helix |
N297Q, I300V, T305S |
12 |
I helix |
CYP2Bs |
|
V183L |
7-8 |
E helix |
Enhanced activity
Altered substrate specificity
Increased protein stability
Enhanced tolerance to organic solvents |
33-37 |
F202A, L209A |
8-9 |
F helix |
K236I |
10-11 |
G helix |
D257N |
10-11 |
G-H loop |
L264F |
11 |
H helix |
L295H |
12 |
I helix |
S334P, P334S |
13-14 |
J-J’ loop |
CYP3A4 |
|
L216W |
8 |
F helix |
Enhanced activity
Altered substrate specificity |
38 |
F228I |
10 |
F-G loop |
|
T433S |
17 |
L-helix |
|
The location of the region is based on CYP X-ray structures and/or models of
individual enzyme, except for CYP2Bs, in which CYP2B4 was used to identify
regions. The CSM number is based on the CSM analysis of CYP2 family performed
earlier (22). The information on functional characterizations of the mutants are
based on earlier studies (last column) using rational and random mutagenesis
approaches. Note that the regions for the same/similar residue numbers in different
families (e.g. 1 vs. 2 vs.) vary more than the regions for the same/similar residue
numbers within the same families or between different subfamilies (e.g. 2A vs. 2B).
Represents between the two CSM or regions; e.g. 8-9 means between CSM 8
and 9. |