Abstract
17β‐N, N‐diethylcarbamoyl‐4‐methyl‐4‐aza‐5α‐an‐drostan‐3‐one (4‐MA) inhibits 5α‐reductase activity in cultured human genital skin fibroblasts. Enzyme kinetic studies analyzed by Eadie‐Hofstee plots demonstrated that 4‐MA is a competitive inhibitor, with an apparent Ki of 15 nM. 4‐MA had a very low binding affinity for the androgen receptor. When fibroblasts were incubated in the presence of testosterone (T) and 4‐MA, nuclear uptake of 5α‐dihydrotestosterone (DHT) decreased in parallel with the inhibition of 5?‐reduc‐tase activity. While the overall sum for the nuclear uptake of T and DHT diminished, the nuclear uptake of T increased. Biological androgen inactivity cannot be precluded on the basis of nuclear T plus DHT uptake. 1984 American Society of Andrology
Original language | English (US) |
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Pages (from-to) | 171-175 |
Number of pages | 5 |
Journal | Journal of andrology |
Volume | 5 |
Issue number | 3 |
DOIs | |
State | Published - 1984 |
Externally published | Yes |
Keywords
- 5?‐reductase
- androgen receptor
- enzyme inhibitor
- fibroblast
- nuclear uptake
ASJC Scopus subject areas
- Endocrinology, Diabetes and Metabolism
- Reproductive Medicine
- Endocrinology
- Urology