Hypocholesterolemic action of the selective estrogen receptor modulator acolbifene in intact and ovariectomized rats with diet-induced hypercholesterolemia

Lemieux, Christian; Gélinas, Yves; Lalonde, Josée; Labrie, Fernand; Richard, Denis; Deshaies, Yves

doi:10.1016/j.metabol.2005.11.016

Cited by 6 publications

(2 citation statements)

References 60 publications

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“…However, the structure of acolbifene is actually similar to that of raloxifene, and unlike fulvestrant, the antiestrogenic side chain of acolbifene does not mask the mutant ER amino acid D351Y to produce an estrogenic action [175]. In addition, acolbifene and EM-800 act as antiestrogens in mammary and uterine tissues, but have estrogenic effects to prevent bone loss and have a favored function in the regulation of lipid metabolism by lowering plasma cholesterol and triglyceride in rodent models [176, 177]. Therefore, acolbifene and EM-800 should be classified as SERMs.…”

Section: New Sermsmentioning

confidence: 99%

Potential of Selective Estrogen Receptor Modulators as Treatments and Preventives of Breast Cancer

Peng¹,

Sengupta²,

Jordan

2009

ACAMC

130

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Estrogen plays vital roles in human health and diseases. Estrogen mediates its actions almost entirely by binding to estrogen receptors (ER), alpha and beta which further function as transcription factors. Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to ER and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers and is also approved as the first chemo-preventive agent for lowering breast cancer incidence in high risk women. The therapeutic and preventive efficacy of tamoxifen was initially proven by series of experiments in the laboratory which laid the foundation of its clinical use. Unfortunately, use of tamoxifen is associated with de-novo and acquired resistance and some undesirable side effects. The molecular study of the resistance provides an opportunity to precisely understand the mechanism of SERM action which may further help in designing new and improved SERMs. Recent clinical studies reveal that another SERM, raloxifene, which is primarily used to treat post-menopausal osteoporosis, is as efficient as tamoxifen in preventing breast cancers with fewer side effects. Overall, these findings open a new horizon for SERMs as a class of drug which not only can be used for therapeutic and preventive purposes of breast cancers but also for various other diseases and disorders. Major efforts are therefore directed to make new SERMs with a better therapeutic profile and fewer side effects.

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Section: New Sermsmentioning

confidence: 99%

Potential of Selective Estrogen Receptor Modulators as Treatments and Preventives of Breast Cancer

Peng¹,

Sengupta²,

Jordan

2009

ACAMC

130

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“…2A-E). Though several mechanisms are suggested for lipid lowering effect of estradiol in postmenopausal hyperlipidemic condition but upregulation of hepatic LDL receptors is the primary means considered to be responsible for the beneficial effect (37,38). The plasma levels of HDL-C "considered to be good cholesterol" were found to be decreased in OVX+HFD fed group.…”

Section: Resultsmentioning

confidence: 96%

Pharmacodynamic Evaluation of Oral Estradiol Nanoparticles in Estrogen Deficient (Ovariectomized) High-Fat Diet Induced Hyperlipidemic Rat Model

et al. 2008

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Evolution of Selective Estrogen and Androgen Receptor Modulators: Status of Current Therapy and New Drug Development

Wurz

DeGregorio

2011

Pharmaceutical Sciences Encyclopedia

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Prior to the discovery of nonsteroidal selective estrogen and androgen receptor modulators (SERMs and SARMs), the only available treatment modalities for conditions such as menopausal symptoms and postmenopausal osteoporosis in women, and the symptoms associated with hypogonadism in men, were steroid based. As this chapter will discuss, recent clinical trial data have shown that the long‐term use of hormone replacement therapy in postmenopausal women is associated with an increased risk of breast cancer and may increase the risk of coronary heart disease and dementia, contrary to the results of previous observational studies. There are also concerns that androgen replacement therapy in hypogonadal men may pose a risk to prostate health, in addition to the difficulties inherent with the delivery of steroidal androgens. Thus, there is now great interest in developing nonsteroidal, orally bioavailable therapies, that is, SERMs and SARMs, that can provide the respective benefits of estrogens and androgens while minimizing their associated side effects.

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Hypocholesterolemic action of the selective estrogen receptor modulator acolbifene in intact and ovariectomized rats with diet-induced hypercholesterolemia

Cited by 6 publications

References 60 publications

Potential of Selective Estrogen Receptor Modulators as Treatments and Preventives of Breast Cancer

Potential of Selective Estrogen Receptor Modulators as Treatments and Preventives of Breast Cancer

Pharmacodynamic Evaluation of Oral Estradiol Nanoparticles in Estrogen Deficient (Ovariectomized) High-Fat Diet Induced Hyperlipidemic Rat Model

Evolution of Selective Estrogen and Androgen Receptor Modulators: Status of Current Therapy and New Drug Development

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