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...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Martinkovich S, Shah D, Planey SL, Arnott JA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Selective Estrogen Receptor Modulators SERMs estrogen receptors Geriatrics RC952-954.6
Acceso en línea:	https://doaj.org/article/8b4abb87201543409684915d5030ff63
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:8b4abb87201543409684915d5030ff63
record_format	dspace
spelling	oai:doaj.org-article:8b4abb87201543409684915d5030ff632021-12-02T11:13:19ZSelective estrogen receptor modulators: tissue specificity and clinical utility1178-1998https://doaj.org/article/8b4abb87201543409684915d5030ff632014-08-01T00:00:00Zhttps://www.dovepress.com/selective-estrogen-receptor-modulators-tissue-specificity-and-clinical-peer-reviewed-article-CIAhttps://doaj.org/toc/1178-1998Stephen 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 receptorsMartinkovich SShah DPlaney SLArnott JADove Medical PressarticleSelective Estrogen Receptor ModulatorsSERMsestrogen receptorsGeriatricsRC952-954.6ENClinical Interventions in Aging, Vol Volume 9, Pp 1437-1452 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Selective Estrogen Receptor Modulators SERMs estrogen receptors Geriatrics RC952-954.6
spellingShingle	Selective Estrogen Receptor Modulators SERMs estrogen receptors Geriatrics RC952-954.6 Martinkovich S Shah D Planey SL Arnott JA Selective estrogen receptor modulators: tissue specificity and clinical utility
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
format	article
author	Martinkovich S Shah D Planey SL Arnott JA
author_facet	Martinkovich S Shah D Planey SL Arnott JA
author_sort	Martinkovich S
title	Selective estrogen receptor modulators: tissue specificity and clinical utility
title_short	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_sort	selective estrogen receptor modulators: tissue specificity and clinical utility
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/8b4abb87201543409684915d5030ff63
work_keys_str_mv	AT martinkovichs selectiveestrogenreceptormodulatorstissuespecificityandclinicalutility AT shahd selectiveestrogenreceptormodulatorstissuespecificityandclinicalutility AT planeysl selectiveestrogenreceptormodulatorstissuespecificityandclinicalutility AT arnottja selectiveestrogenreceptormodulatorstissuespecificityandclinicalutility
_version_	1718396117983428608

Selective estrogen receptor modulators: tissue specificity and clinical utility

Ejemplares similares