Selective estrogen receptor modulators: tissue specificity and clinical utility
Stephen Martinkovich,* Darshan Shah,* Sonia Lobo Planey, John A ArnottDepartment of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA*These authors contributed equally to this workAbstract: Selective estrogen receptor modulators (SERMs) are a diverse group of ­nonsteroidal...
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2014-08-01
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| Series: | Clinical Interventions in Aging |
| Subjects: | |
| Online Access: | https://www.dovepress.com/selective-estrogen-receptor-modulators-tissue-specificity-and-clinical-peer-reviewed-article-CIA |
| _version_ | 1828975357656563712 |
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| author | Martinkovich S Shah D Planey SL Arnott JA |
| author_facet | Martinkovich S Shah D Planey SL Arnott JA |
| author_sort | Martinkovich S |
| collection | DOAJ |
| description | Stephen Martinkovich,* Darshan Shah,* Sonia Lobo Planey, John A ArnottDepartment of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA*These authors contributed equally to this workAbstract: Selective estrogen receptor modulators (SERMs) are a diverse group of ­nonsteroidal compounds that function as agonists or antagonists for estrogen receptors (ERs) in a target gene-specific and tissue-specific fashion. SERM specificity involves tissue-specific expression of ER subtypes, differential expression of co-regulatory proteins in various tissues, and varying ER conformational changes induced by ligand binding. To date, the major clinical applications of SERMs are their use in the prevention and treatment of breast cancer, the prevention of osteoporosis, and the maintenance of beneficial serum lipid profiles in postmenopausal women. However, SERMs have also been found to promote adverse effects, including thromboembolic events and, in some cases, carcinogenesis, that have proven to be obstacles in their clinical utility. In this review, we discuss the mechanisms of SERM tissue specificity and highlight the therapeutic application of well-known and emergent SERMs.Keywords: selective estrogen receptor modulators, SERMs, estrogen receptors |
| first_indexed | 2024-12-14T14:18:42Z |
| format | Article |
| id | doaj.art-8b4abb87201543409684915d5030ff63 |
| institution | Directory Open Access Journal |
| issn | 1178-1998 |
| language | English |
| last_indexed | 2024-12-14T14:18:42Z |
| publishDate | 2014-08-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Clinical Interventions in Aging |
| spelling | doaj.art-8b4abb87201543409684915d5030ff632022-12-21T22:58:08ZengDove Medical PressClinical Interventions in Aging1178-19982014-08-01Volume 91437145218118Selective estrogen receptor modulators: tissue specificity and clinical utilityMartinkovich SShah DPlaney SLArnott JAStephen Martinkovich,* Darshan Shah,* Sonia Lobo Planey, John A ArnottDepartment of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA*These authors contributed equally to this workAbstract: Selective estrogen receptor modulators (SERMs) are a diverse group of ­nonsteroidal compounds that function as agonists or antagonists for estrogen receptors (ERs) in a target gene-specific and tissue-specific fashion. SERM specificity involves tissue-specific expression of ER subtypes, differential expression of co-regulatory proteins in various tissues, and varying ER conformational changes induced by ligand binding. To date, the major clinical applications of SERMs are their use in the prevention and treatment of breast cancer, the prevention of osteoporosis, and the maintenance of beneficial serum lipid profiles in postmenopausal women. However, SERMs have also been found to promote adverse effects, including thromboembolic events and, in some cases, carcinogenesis, that have proven to be obstacles in their clinical utility. In this review, we discuss the mechanisms of SERM tissue specificity and highlight the therapeutic application of well-known and emergent SERMs.Keywords: selective estrogen receptor modulators, SERMs, estrogen receptorshttps://www.dovepress.com/selective-estrogen-receptor-modulators-tissue-specificity-and-clinical-peer-reviewed-article-CIASelective Estrogen Receptor ModulatorsSERMsestrogen receptors |
| spellingShingle | Martinkovich S Shah D Planey SL Arnott JA Selective estrogen receptor modulators: tissue specificity and clinical utility Clinical Interventions in Aging Selective Estrogen Receptor Modulators SERMs estrogen receptors |
| title | Selective estrogen receptor modulators: tissue specificity and clinical utility |
| title_full | Selective estrogen receptor modulators: tissue specificity and clinical utility |
| title_fullStr | Selective estrogen receptor modulators: tissue specificity and clinical utility |
| title_full_unstemmed | Selective estrogen receptor modulators: tissue specificity and clinical utility |
| title_short | Selective estrogen receptor modulators: tissue specificity and clinical utility |
| title_sort | selective estrogen receptor modulators tissue specificity and clinical utility |
| topic | Selective Estrogen Receptor Modulators SERMs estrogen receptors |
| url | https://www.dovepress.com/selective-estrogen-receptor-modulators-tissue-specificity-and-clinical-peer-reviewed-article-CIA |
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