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Selective estrogen receptor modulators: tissue specificity and clinical utility

Authors Martinkovich S, Shah D, Planey SL, Arnott J

Received 23 April 2014

Accepted for publication 22 May 2014

Published 28 August 2014 Volume 2014:9 Pages 1437—1452


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Stephen Martinkovich,* Darshan Shah,* Sonia Lobo Planey, John A Arnott

Department of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA

*These authors contributed equally to this work

Abstract: 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

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