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  • Pre-receptor regulation of the androgen receptor
    Penning, Trevor M. ...
    The human androgen receptor (AR) is a ligand-activated nuclear transcription factor and mediates the induction of genes involved in the development of the male phenotype and male secondary sex ... characteristics, as well as the normal and abnormal growth of the prostate. We have identified the pair of bydroxysteroid dehydrogenases (HSDs) that regulate ligand access to the AR in human prostate. We find that type 3 3alpha-HSD (aldo-keto reductase (AKR)IC2) catalyzes the NADPH dependent reduction of the potent androgen Sa-dihydrotestosterone (5alpha-DHT) to yield the inactive androgen 3alpha-androstanediol (3alpha-diol). We also find that RoDH like 3alpha-HSD (RL-HSD) catalyzes the NAD+ dependent oxidation of 3alpha-diol to yield 5alpha-DHT. Together these enzymes are involved in the pre-receptor regulationof androgen action. Inhibition of AKR1C2 would be desirable in casesof androgen insufficiency and inhibition of RL-HSD might be desirable in benign prostatic hyperplasia.
    Vrsta gradiva - članek, sestavni del
    Leto - 2008
    Jezik - angleški
    COBISS.SI-ID - 23711449