title: Selective estrogen receptor modulators: tissue specificity and clinical utility.
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.
authors.affiliation: Department of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA.
authors.forename: Stephen
authors.initials: S
authors.lastname: Martinkovich
authors.affiliation: Department of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA.
authors.forename: Darshan
authors.initials: D
authors.lastname: Shah
authors.affiliation: Department of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA.
authors.forename: Sonia Lobo
authors.initials: SL
authors.lastname: Planey
authors.affiliation: Department of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA.
authors.forename: John A
authors.initials: JA
authors.lastname: Arnott
mesh_terms: D005260:Female; D006801:Humans; D009928:Organ Specificity; D020845:Selective Estrogen Receptor Modulators / Q000009:adverse effects / Q000627:therapeutic use*
chemical_list: D020845:Selective Estrogen Receptor Modulators
keywords: SERMs; estrogen receptors; selective estrogen receptor modulators