Human estrogen receptor beta-gene structure, chromosomal localization, and expression pattern.
Eva Enmark,Markku Pelto-Huikko,Markku Pelto-Huikko,Kaj Grandien,Svetlana Lagercrantz,Jacob Lagercrantz,Gabriel Fried,Magnus Nordenskjöld,Jan-Åke Gustafsson +8 more
TL;DR: Data regarding the genomic structure and chromosomal localization of the human ERβ gene is presented, demonstrating that two independent ER genes do exist in the human and that this receptor is expressed in multiple tissues.
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Abstract: The estrogen receptor (ER) is a ligand-activated transcription factor that mediates the effects of the steroid hormone 17 beta-estradiol, in both males and females. Since the isolation and cloning of ER, the consensus has been that only one such receptor exists. The finding of a second subtype of ER (ER beta) has caused considerable excitement amongst endocrinologists. In this article, we present data regarding the genomic structure and chromosomal localization of the human ER beta gene, demonstrating that two independent ER genes do exist in the human. Furthermore, we present data regarding the tissue distribution of human ER beta, showing that this receptor is expressed in multiple tissues. For instance, ER beta is found in developing spermatids of the testis, a finding of potential relevance for the ongoing debate on the effects of environmental estrogens on sperm counts. In addition, we find ER beta in ovarian granulosa cells, indicating that estrogens also participate in the regulation of follicular growth in the human.
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Citations
Ligand-, Cell-, and Estrogen Receptor Subtype (α/β)-dependent Activation at GC-rich (Sp1) Promoter Elements
Brad Saville,Mark Wormke,Fan Wang,Thu Annelise Nguyen,Eva Enmark,George G.J.M. Kuiper,Jan-Åke Gustafsson,Stephen Safe +7 more
TL;DR: Exchange of activation function-1 (AF-1) domains of ER subtypes gave chimeric ERα/β and ERβ/α proteins that resembled wild-type ER in terms of physical association with Sp1 protein, and transactivation studies indicated that the region between amino acids 79 and 117 of this domain is important for activation at an Sp1 element.
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Molecular mechanism of estrogen-estrogen receptor signaling.
TL;DR: A better understanding of the complex regulatory mechanisms that underlie ER actions in response to E2 holds a critical trajectory for the development of novel prognostic and therapeutic approaches with substantial impacts on the systemic management of target tissue diseases.
408
•Journal Article
Expression of estrogen receptor (ER) subtypes and ERbeta isoforms in colon cancer.
TL;DR: Data show that ERbeta is the predominant ER subtype in the human colon and that decreased levels of ER beta1 and ERbeta2 mRNA are associated with colonic tumorigenesis in females, which suggests that activation of ERbeta-mediated processes in the superficial colonic epithelium may have a role in the preventive effects observed for female gender and ERT usage.
405
Estradiol acts as a germ cell survival factor in the human testis in vitro.
TL;DR: The novel findings of the present study together with the previously reported indirect effects of estrogens on male germ cells indicate the importance of estrogen for the normal function of the testis.
Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment.
Hitisha K. Patel,Teeru Bihani +1 more
TL;DR: This review discusses various ER antagonists investigated for the treatment of breast cancer, outlining their pharmacological and tissue-specific mechanisms of action as well as their specified use within the ER+ breast cancer setting.
402
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