Estren is a selective estrogen receptor modulator with transcriptional activity.
Artikel i vetenskaplig tidskrift, 2003

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.

genetics

Drug

Genetic

Dose-Response Relationship

drug effects

Inbred C57BL

Mice

Mice

Bone and Bones

metabolism

drug effects

metabolism

Female

metabolism

Mice

metabolism

Humans

Ovariectomy

drug effects

pharmacology

metabolism

Estrogen

Uterus

Transgenic

Transcription

physiology

pharmacology

Male

agonists

Animals

Estrogen Receptor Modulators

Receptors

Estrenes

Författare

Sofia Movérare-Skrtic

Göteborgs universitet

Johanna Dahllund

Niklas Andersson

Göteborgs universitet

Ulrika Islander

Göteborgs universitet

Catharina Lindholm

Göteborgs universitet

Jan-Ake Gustafsson

Stefan Nilsson

Claes Ohlsson

Göteborgs universitet

Molecular Pharmacology

0026-895X (ISSN) 1521-0111 (eISSN)

Vol. 64 6 1428-33

Ämneskategorier

MEDICIN OCH HÄLSOVETENSKAP

DOI

10.1124/mol.64.6.1428

PubMed

14645673