Title |
Selective estrogen receptor modulators: tissue specificity and clinical utility
|
---|---|
Published in |
Clinical Interventions in Aging, August 2014
|
DOI | 10.2147/cia.s66690 |
Pubmed ID | |
Authors |
Stephen Martinkovich, Darshan Shah, Sonia Lobo Planey, John A Arnott |
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. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 214 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 36 | 17% |
Student > Bachelor | 36 | 17% |
Student > Master | 30 | 14% |
Researcher | 19 | 9% |
Student > Doctoral Student | 14 | 7% |
Other | 34 | 16% |
Unknown | 45 | 21% |
Readers by discipline | Count | As % |
---|---|---|
Biochemistry, Genetics and Molecular Biology | 41 | 19% |
Medicine and Dentistry | 29 | 14% |
Agricultural and Biological Sciences | 28 | 13% |
Pharmacology, Toxicology and Pharmaceutical Science | 26 | 12% |
Chemistry | 12 | 6% |
Other | 24 | 11% |
Unknown | 54 | 25% |