Interaction of Androst-5-ene-3 beta,17 beta-diol and 5 alpha-androstane-3 beta,17 beta-diol with estrogen and androgen receptors: A combined binding and cell study
文献类型：期刊论文
| 作者 | Chen, J; Wang, WQ; Lin, SX |
| 刊名 | JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
 |
| 出版日期 | 2013 |
| 卷号 | 137期号:1页码:316-321 |
| 关键词 | Estrogens Androgens Estrogen receptors Antiestrogens Antiandrogens Ligands |
| 通讯作者 | Lin, SX (reprint author), CHU, Quebec Res Ctr CHUL, Lab Mol Endocrinol & Oncol, Quebec City, PQ G1V 4G2, Canada.,sxlin@crchul.ulaval.ca |
| 英文摘要 | Androst-5-ene-3 beta,17 beta-diol (ADIOL) and 5 alpha-androstane-3 beta,17 beta-diol (3 beta-DIOL), metabolites of dehydroepiandrosterone (DHEA) and dihydrotestosterone (DHT), respectively, are known to possess estrogenic properties. To better understand their hormonal action and roles in the proliferation of breast cancer (BC) cells, we studied their binding to sex-hormone receptors in estrogen receptor (ER)-positive (ZR-75-1 and T-47D) and ER-negative (MDA-MB-231) human BC cells. The results demonstrated that estradiol (E-2), ADIOL and 3 beta-DIOL stimulated the proliferation of ZR-75-1 and T-47D cells, but had no effect on ER-negative cells. In the presence of estradiol, ADIOL and 3 beta-DIOL inhibited the estrogen-stimulated BC cell growth. This inhibition was counteracted by anti-androgens, which were unable to affect the ADIOL and 3 beta-DIOL stimulatory effects in E2 -free medium. On the other hand, in the presence of tamoxifen, ADIOL and 3 beta-DIOL showed an additional anti-proliferative activity on hormone-sensitive BC cells compared with tamoxifen treatment alone. These results are similar to previous reports obtained using MCF-7 cells, which confirmed that ADIOL and 3 beta-DIOL stimulated estrogen-dependent BC cell growth via ERs, but inhibited growth via androgen receptors (ARs). Several steroids bind to both ER and AR in a different preference and degree, i.e. E-2 > estrone (Er) > ADIOL > 3 beta-DIOL> testosterone (T)> DHT for ER and DHT>T>3 beta-DIOL>ADIOL> E-1 > E-2 for AR. The relative binding affinities of ADIOL, 3 beta-DIOL, and E2 corresponded well to their respective potential in stimulating cell proliferation of ZR-75-1 and T-47D cells in our results. The intrinsic relationship between cell proliferation effects and binding affinities for receptors of several steroids was revealed here by a combined binding and cell study. This article is part of a Special Issue entitled 'Synthesis and biological testing of steroid derivatives as inhibitors'. (C) 2013 Published by Elsevier Ltd. |
| 学科主题 | Biochemistry & Molecular Biology ; Endocrinology & Metabolism |
| 类目[WOS] | Biochemistry & Molecular Biology ; Endocrinology & Metabolism |
| 关键词[WOS] | HUMAN-BREAST-CANCER ; GROWTH ; MCF-7 ; PROLIFERATION ; STIMULATION ; 17-BETA-DIOL |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000327048400026 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/507]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Chen, J,Wang, WQ,Lin, SX. Interaction of Androst-5-ene-3 beta,17 beta-diol and 5 alpha-androstane-3 beta,17 beta-diol with estrogen and androgen receptors: A combined binding and cell study[J]. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,2013,137(1):316-321. |
| APA | Chen, J,Wang, WQ,&Lin, SX.(2013).Interaction of Androst-5-ene-3 beta,17 beta-diol and 5 alpha-androstane-3 beta,17 beta-diol with estrogen and androgen receptors: A combined binding and cell study.JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,137(1),316-321. |
| MLA | Chen, J,et al."Interaction of Androst-5-ene-3 beta,17 beta-diol and 5 alpha-androstane-3 beta,17 beta-diol with estrogen and androgen receptors: A combined binding and cell study".JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY 137.1(2013):316-321. |
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