Application | Comment | Organism |
---|---|---|
medicine | 30 min incubation with dutasteride results in the lowest apparent Ki values overall and the lowest variation, significant for designing protocols for treatment and/or chemoprevention of prostatic diseases | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
A248V | somatic variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
A49T | constitutional and somatic variant, time-independent inhibition, more than 100fold lower apparent Ki for dutasteride than for finasteride | Homo sapiens |
A51T | constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
C5R | constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
F118L | somatic variant, no significant change of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
F194L | constitutional variant, time-independent inhibition, displays lower apparent Ki for finasteride than dutasteride | Homo sapiens |
F234L | constitutional variant, reduction of the apparent Ki for finasteride but not for dutasteride | Homo sapiens |
G183D | somatic variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
G191E | somatic variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
L221P | somatic variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
L226P | somatic variant, reduction of the apparent Ki for finasteride but not for dutasteride | Homo sapiens |
P30L | constitutional variant, more than 100fold lower apparent Ki for dutasteride than for finasteride | Homo sapiens |
P48R | constitutional variant, displays lower apparent Ki for finasteride than dutasteride in the 10 min reaction | Homo sapiens |
R227Q | constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
T187M | constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
V189A | somatic variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
V3I | somatic variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
V63M | somatic variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
V89L | constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
dutasteride | slow, time-dependent inhibitor, more efficient than finasteride | Homo sapiens | |
finasteride | slow, time-dependent inhibitor | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
prostate gland | - |
Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
steroid 5alpha-reductase | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | the majority of the enzyme variants result in a reduction of the apparent Ki for both finasteride and dutasteride from 10 min to the 30 min reaction like the wild-type enzyme, but several variants result in an increase of the apparent Ki for each inhibitor or no significant change between the 10 min and 30 min reactions, thus exhibiting time independent inhibition | Homo sapiens | |
0.0000043 | - |
dutasteride | wild-type, 30 min reaction time | Homo sapiens | |
0.000017 | - |
dutasteride | wild-type, 10 min reaction time | Homo sapiens | |
0.000023 | - |
finasteride | wild-type, 30 min reaction time | Homo sapiens | |
0.00006 | - |
finasteride | wild-type, 10 min reaction time | Homo sapiens |