Tamoxifen and Endometrial Cancer: A Janus-Headed Drug
Tamoxifen is a selective estrogen receptor modulator used for the treatment and prevention of estrogen receptor (ER)—positive breast cancer. However, tamoxifen increases the risk of endometrial cancer (EC) by about 2–7 fold, and more aggressive types of EC with poor prognoses are observed in tamoxif...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-09-01
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| Series: | Cancers |
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| Online Access: | https://www.mdpi.com/2072-6694/12/9/2535 |
| _version_ | 1797554447097790464 |
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| author | Günter Emons Alexander Mustea Clemens Tempfer |
| author_facet | Günter Emons Alexander Mustea Clemens Tempfer |
| author_sort | Günter Emons |
| collection | DOAJ |
| description | Tamoxifen is a selective estrogen receptor modulator used for the treatment and prevention of estrogen receptor (ER)—positive breast cancer. However, tamoxifen increases the risk of endometrial cancer (EC) by about 2–7 fold, and more aggressive types of EC with poor prognoses are observed in tamoxifen users. On the other hand, tamoxifen is an efficacious treatment for advanced or recurrent EC with low toxicity. The differential agonistic or antagonistic effects of tamoxifen on ERα are explained by the tissue-specific expression profiles of co-activators and co-repressors of the receptor. The estrogen-agonistic effect of tamoxifen in endometrial cancers can also be explained by the expression of G-protein coupled estrogen receptor 1 (GPER-1), a membrane-bound estrogen receptor for which tamoxifen and other “antiestrogens” are pure agonists. |
| first_indexed | 2024-03-10T16:32:13Z |
| format | Article |
| id | doaj.art-c3020f5326354c62b92e383aaf5f6109 |
| institution | Directory Open Access Journal |
| issn | 2072-6694 |
| language | English |
| last_indexed | 2024-03-10T16:32:13Z |
| publishDate | 2020-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cancers |
| spelling | doaj.art-c3020f5326354c62b92e383aaf5f61092023-11-20T12:48:02ZengMDPI AGCancers2072-66942020-09-01129253510.3390/cancers12092535Tamoxifen and Endometrial Cancer: A Janus-Headed DrugGünter Emons0Alexander Mustea1Clemens Tempfer2Department of Obstetrics and Gynecology, Georg-August-University, 37075 Göttingen, GermanyDepartment of Gynecology and Gynecological Oncology, University Hospital, 53127 Bonn, GermanyDepartment of Obstetrics and Gynecology, Ruhr University, 44625 Herne, GermanyTamoxifen is a selective estrogen receptor modulator used for the treatment and prevention of estrogen receptor (ER)—positive breast cancer. However, tamoxifen increases the risk of endometrial cancer (EC) by about 2–7 fold, and more aggressive types of EC with poor prognoses are observed in tamoxifen users. On the other hand, tamoxifen is an efficacious treatment for advanced or recurrent EC with low toxicity. The differential agonistic or antagonistic effects of tamoxifen on ERα are explained by the tissue-specific expression profiles of co-activators and co-repressors of the receptor. The estrogen-agonistic effect of tamoxifen in endometrial cancers can also be explained by the expression of G-protein coupled estrogen receptor 1 (GPER-1), a membrane-bound estrogen receptor for which tamoxifen and other “antiestrogens” are pure agonists.https://www.mdpi.com/2072-6694/12/9/2535tamoxifenendometrial cancerselective estrogen receptor modulator |
| spellingShingle | Günter Emons Alexander Mustea Clemens Tempfer Tamoxifen and Endometrial Cancer: A Janus-Headed Drug Cancers tamoxifen endometrial cancer selective estrogen receptor modulator |
| title | Tamoxifen and Endometrial Cancer: A Janus-Headed Drug |
| title_full | Tamoxifen and Endometrial Cancer: A Janus-Headed Drug |
| title_fullStr | Tamoxifen and Endometrial Cancer: A Janus-Headed Drug |
| title_full_unstemmed | Tamoxifen and Endometrial Cancer: A Janus-Headed Drug |
| title_short | Tamoxifen and Endometrial Cancer: A Janus-Headed Drug |
| title_sort | tamoxifen and endometrial cancer a janus headed drug |
| topic | tamoxifen endometrial cancer selective estrogen receptor modulator |
| url | https://www.mdpi.com/2072-6694/12/9/2535 |
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