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Estren Is a Selective Estrogen Receptor Modulator with Transcriptional Activity

Center for Bone Research at the Sahlgrenska Academy, Department of Internal Medicine, the Sahlgrenska Academy at Göteborg University, Göteborg, Sweden (S.M., N.A., U.I., H.C., C.O.); Karo Bio AB, Novum, Huddinge, Sweden (J.D., S.N.); and Department of Biosciences at Novum and Department of Medical Nutrition, Karolinska Institutet, Novum, Huddinge, Sweden (J.-Å.G.)

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 ER- and ER-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 17-estradiol for both ER and ER. Thus, estren has the capacity to exert genomic effects via both ER and ER. We conclude, in contrast to what was previously reported by others, that estren is a SERM with transcriptional activity.

Address correspondence to: Dr. Claes Ohlsson, Department of Internal Medicine, Division of Endocrinology, Gröna Stråket 8, 413 45 Gothenburg, Sweden. E-mail: claes.ohlsson{at}medic.gu.se

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