Estren is a selective estrogen receptor modulator with transcriptional activity.

• 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.

Keyword

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

genetics

Publication and Content Type

ref (subject category)

art (subject category)