Pre-Receptor Regulation of the Androgen Receptor
January 2008
in “
Molecular and cellular endocrinology
”
TLDR Two enzymes regulate androgen receptor activity, affecting treatments for androgen insufficiency and benign prostatic hyperplasia.
The study identified two hydroxysteroid dehydrogenases (HSDs) that regulate ligand access to the androgen receptor (AR) in the human prostate. Type 3 3α-HSD (AKR1C2) reduced the potent androgen 5α-dihydrotestosterone (5α-DHT) to the inactive 3α-androstanediol (3α-diol) using NADPH, while RoDH-like 3α-HSD (RL-HSD) oxidized 3α-diol back to 5α-DHT using NAD+. These enzymes played a role in pre-receptor regulation of androgen action, suggesting that inhibiting AKR1C2 could be beneficial in androgen insufficiency, and inhibiting RL-HSD could be useful in treating benign prostatic hyperplasia.
