scholarly journals NEW APPROACHES TO OSTEOPOROSIS IN PRIMARY CARE

2017 ◽  
Vol 12 (4) ◽  
pp. 184-191
Author(s):  
Mihaela Daniela BALTĂ ◽  
◽  
Mihaela Adela IANCU ◽  
Dumitru MATEI ◽  
◽  
...  
Keyword(s):  
Hormone Replacement ◽  
Adherence To Treatment ◽  
Treatment Of Osteoporosis ◽  
Estrogen Receptor Modulators ◽  
Aging Populations ◽  
Receptor Modulators ◽  
Current Guidelines ◽  
Frax Score ◽  
Insight Into

Osteoporosis is a disease that affects an increasing number of people, given the tendency of aging populations. Fragile bone and increases risk of bones breaking, their consequences, impairment of quality of life have prompted health policies to provide a greater insight into this condition. It is important to identify the risk factors and start the preventive and curative treatment as early as possible. Current guidelines recommend using the FRAX score to determine the risk of major fracture over the next 10 years, followed by DXA determination. The current guidelines highlight the importance of non-medication measures, calcium and vitamin D intake. Among the therapeutic agents used in the treatment of osteoporosis, the first line are bisphosphonates poor, in case of intolerance, bisphosphonates iv or antibodies anti RANKL (denosumab). Selective estrogen receptor modulators and hormone replacement therapy are not routinely indicated, and recombinant PTH is expensive and is intended for severe and resistant forms. The adherence to treatment is poor, so we need measures to increase prevention, screening and early treatment of osteoporosis, as well as measures to educate the population.

New Therapies for Osteoporosis

2008 ◽  
Vol 22 (1) ◽  
pp. 53-64
Author(s):  
Karly A. Hegge ◽  
Anisa S. Fornoff ◽  
Sheryl L. Gutierres ◽  
Sally L. Haack
Keyword(s):  
Therapeutic Option ◽  
Sequential Therapy ◽  
The United States ◽  
Health Concern ◽  
Treatment Of Osteoporosis ◽  
Estrogen Receptor Modulators ◽  
Osteoporosis In Men ◽  
Surrogate Measures ◽  
Receptor Modulators

Osteoporosis is a growing health concern in the United States, with an enormous impact on morbidity and mortality. Despite published guidelines to aid clinicians in its management, several controversies remain. Many trials evaluate surrogate measures of bone strength rather than more clinically relevant outcomes, including fracture. Furthermore, the role of combination and sequential therapy remains unclear. Limited data are available regarding appropriate duration of therapy, management of osteoporosis in men, and treatment of glucocorticoid-induced osteoporosis. The development of unique therapeutic agents could potentially revolutionize the treatment of osteoporosis. Once yearly zoledronic acid may provide advantages over existing therapies. Because of limitations with existing selective estrogen receptor modulators, the search for agents with better efficacy and safety profiles has led to the development of several new medications within this class. Finally, denosumab, a monoclonal antibody to receptor activator for nuclear factor-kappa B ligand, also represents a novel therapeutic option for osteoporosis.

scholarly journals Ligand-Selective Interdomain Conformations of Estrogen Receptor-α

2007 ◽  
Vol 21 (1) ◽  
pp. 49-61 ◽  
Author(s):  
Adrian Padron ◽  
Li Li ◽  
Eric M. Kofoed ◽  
Fred Schaufele
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Energy Transfer ◽  
Hormone Replacement ◽  
Estrogen Receptor Α ◽  
Full Length ◽  
Estrogen Receptor Modulators ◽  
Interaction Kinetics ◽  
Receptor Modulators

Abstract Selective estrogen receptor modulators (SERMs) inhibit estrogen activation of the estrogen receptor (ER) in some tissues but activate ER in other tissues. These tissue-selective actions suggest that SERMs may be identified with tissue specificities that would improve the safety of breast cancer and hormone replacement therapies. The identification of an improved SERM would be aided by understanding the effects of each SERM on the structure and interactions of ER. To date, the inability to obtain structures of the full-length ER has limited our structural characterization of SERM action to their antiestrogenic effects on the isolated ER ligand binding domain. We studied the effects of estradiol and the clinically useful SERMs 4-hydroxytamoxifen and fulvestrant on the conformation of the full-length ERα dimer complex by comparing, in living human breast cancer cells, the amounts of energy transfer between fluorophores attached to different domains of ERα. Estradiol, 4-hydroxytamoxifen, and fulvestrant all promoted the rapid formation of ERα dimers with equivalent interaction kinetics. The amino- and carboxyl-terminal ERα domains both contain activation functions differentially affected by these ligands, but the positions of only the carboxyl termini differed upon binding with estradiol, 4-hydroxytamoxifen, or fulvestrant. The association of a specific ERα dimer conformation with the binding of ligands of different clinical effect will assist the identification of a SERM with optimal tissue-selective estrogenic and antiestrogenic activities. These studies also provide a roadmap for dissecting important structural and kinetic details for any protein complex from the quantitative analysis of energy transfer.

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