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  • Expression of human aldo-keto reductase 1C2 in cell lines of peritoneal endometriosis: potential implications in metabolism of progesterone and dydrogesterone and inhibition by progestins
    Beranič, Nataša, 1985- ...
    The human aldo-keto reductase AKR1C2 converts 5[alpha]-dihydrotestosterone to the less active 3[alpha]-androstanediol and has a minor 20-ketosteroid reductase redactivity that metabolises ... progesterone to 20[alpha] -hydroxyprogesterone. AKR1C2 is expressed in different peripheral tissues, but its role in uterine diseases like endometriosis has not been studied in detail. Some progestins used for treatment of endometriosis inhibit AKR1C1 and AKR1C3, with unknown effects on AKR1C2. In this study we investigated expression of AKR1C2 in the model cell lines of peritoneal endometriosis, and examined the ability of recombinant AKR1C2 to metabolise progesterone and progestin dydrogesterone, as well as itspotential inhibition by progestins. AKR1C2 is expressed in epithelial and stromal endometriotic cell lines at the mRNA level. The recombinant enzyme catalyses reduction of progesterone to 20?-hydroxyprogesterone with a 10-fold lower catalytic efficiency than the major 20-ketosteroid reductase, AKR1C1. AKR1C2 also metabolises progestin dydrogesterone to its 20[alpha]-dihydrodydrogesterone, with 8.6-fold higher catalytic efficiency than 5[alpha]-dihydrotestosterone. Among the progestins that are currently used for treatment of endometriosis, dydrogesterone, medroxyprogesterone acetate and 20[alpha]-dihydrodydrogesterone act as AKR1C2 inhibitors with low [micro]M Ki values in vitro. Their potential in vivo effects should be further studied.
    Vir: Journal of Steroid Biochemistry and Molecular Biology. - ISSN 0960-0760 (Vol. 130, iss. 1-2, 2012, str. 16-25)
    Vrsta gradiva - članek, sestavni del
    Leto - 2012
    Jezik - angleški
    COBISS.SI-ID - 3193713

    Povezava(-e):

    http://www.sciencedirect.com/science/article/pii/S0960076011002536
    DOI

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