Estren is a selective estrogen receptor modulator with transcriptional activity.
Journal article, 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.
Transcription
Mice
Dose-Response Relationship
pharmacology
Estrogen Receptor Modulators
Genetic
drug effects
Inbred C57BL
physiology
metabolism
Mice
Mice
metabolism
genetics
Transgenic
Bone and Bones
pharmacology
Estrogen
drug effects
Estrenes
Ovariectomy
Uterus
Humans
Receptors
Drug
drug effects
Female
agonists
Animals
metabolism
Male
metabolism
metabolism
Author
Sofia Movérare-Skrtic
University of Gothenburg
Johanna Dahllund
Niklas Andersson
University of Gothenburg
Ulrika Islander
University of Gothenburg
Catharina Lindholm
University of Gothenburg
Jan-Ake Gustafsson
Stefan Nilsson
Claes Ohlsson
University of Gothenburg
Molecular Pharmacology
0026-895X (ISSN) 1521-0111 (eISSN)
Vol. 64 6 1428-33Subject Categories (SSIF 2011)
MEDICAL AND HEALTH SCIENCES
DOI
10.1124/mol.64.6.1428
PubMed
14645673