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Estren is a selective estrogen receptor modulator with transcriptional activity.

Författare och institution:
Sofia Movérare (Institutionen för invärtesmedicin); Johanna Dahllund (-); Niklas Andersson (Institutionen för invärtesmedicin, Avdelningen för internmedicin); Ulrika Islander (Institutionen för invärtesmedicin, Avdelningen för reumatologi och inflammationsforskning); Hans Carlsten (Institutionen för invärtesmedicin, Avdelningen för reumatologi och inflammationsforskning); Jan-Ake Gustafsson (-); Stefan Nilsson (-); Claes Ohlsson (Institutionen för invärtesmedicin, Avdelningen för internmedicin)
Publicerad i:
Molecular pharmacology, 64 ( 6 ) s. 1428-33
Artikel, refereegranskad vetenskaplig
Sammanfattning (abstract):
It was recently reported that the synthetic compound estren increases bone mass without affecting reproductive organs or classic transcription. The aim of the present study was to further characterize the in vivo and in vitro effects of estren. We demonstrate that estren is a selective estrogen receptor modulator (SERM) with a strong effect on thymus, a moderate effect on uterus and trabecular bone, but no major effect on fat or cortical bone in 11-month-old ovariectomized mice. The effect of estren on trabecular bone and uterus is mediated via estrogen receptors (ERs) because no effect is seen in ER double-inactivated mice. Furthermore, with the use of ERalpha- and ERbeta-expressing reporter cell lines, we demonstrate that estren displays an agonistic effect on transcriptional activity of an estrogen-responsive element-driven reporter gene with a degree of agonism similar to that of 17beta-estradiol for both ERalpha and ERbeta. Thus, estren has the capacity to exert genomic effects via both ERalpha and ERbeta. We conclude, in contrast to what was previously reported by others, that estren is a SERM with transcriptional activity.
Ämne (baseras på Högskoleverkets indelning av forskningsämnen):
Animals, Bone and Bones, drug effects, metabolism, Dose-Response Relationship, Drug, Estrenes, metabolism, pharmacology, Estrogen Receptor Modulators, metabolism, pharmacology, Female, Humans, Male, Mice, Mice, Inbred C57BL, Mice, Transgenic, Ovariectomy, Receptors, Estrogen, agonists, genetics, metabolism, Transcription, Genetic, drug effects, physiology, Uterus, drug effects, metabolism
Postens nummer:
Posten skapad:
2008-10-14 07:44
Posten ändrad:
2011-01-20 09:59

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