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Literature summary for 1.3.1.22 extracted from

  • Makridakis, N.; Reichardt, J.K.
    Pharmacogenetic analysis of human steroid 5alpha reductase type II: Comparison of finasteride and dutasteride (2005), J. Mol. Endocrinol., 34, 617-623.
    View publication on PubMed
Search for more literature for 1.3.1.22

Application

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

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

Inhibitors Comment Organism Structure
dutasteride slow, time-dependent inhibitor, more efficient than finasteride Homo sapiens
finasteride slow, time-dependent inhibitor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
prostate gland
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
steroid 5alpha-reductase
-
 Homo sapiens

Ki Value [mM]

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