scholarly journals Tamoxifen non-estrogen receptor mediated molecular targets

2012 ◽  
Vol 6 (2) ◽  
pp. 15 ◽  
Author(s):  
Tatiana Bogush ◽  
Evgeny Dudko ◽  
Elena Bogush ◽  
Boris Polotsky ◽  
Sergei Tjulandin ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Biological Activities ◽  
Biological Effects ◽  
Experimental Studies ◽  
Estrogen Receptor Beta ◽  
Point Of View ◽  
Tamoxifen Treatment ◽  
Cellular Targets

Recent experimental studies revealing new biological effects of tamoxifen on tumor cells both expressing and not expressing different types of estrogen receptors (ERα and ERβ) show new aspects of a seemingly well known agent. This review describes tamoxifen targets, the blocking of which leads to inhibition of tumor cell growth and angiogenesis, stimulation of programmed cell death (apoptosis, autophagia and necrosis), inhibition of multidrug resistance, invasion and metastasis. Since outcomes of tamoxifen action on cells are prognostically good from the point of view of both tumor growth/metastasis inhibition and tumor response to drug therapy, the authors believe this is an extremely important addition to tamoxifen antiestrogenic effect. Arguments are provided to consider the strategy of long-term tamoxifen treatment proposed by Professor Craig V. Jordan in the 1970s that is also applicable to the treatment of other tumors. This is, first of all, the fact that expression of estrogen receptor-beta that can also be targeted by tamoxifen therapy in solid tumors of practically all known sites and histologies. The authors believe that molecular biological screening of patients with respect to expression of tamoxifen cellular targets other than ERα and ERβ is needed to use to the full all tamoxifen biological activities other than modulation of estrogen receptors during long-term adjuvant therapy for cancers of various sites.

scholarly journals Tamoxifen non-estrogen receptor mediated molecular targets

2012 ◽  
pp. e15
Author(s):  
Tatiana Bogush ◽  
Evgeny Dudko ◽  
Elena Bogush ◽  
Boris Polotsky ◽  
Sergei Tjulandin ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Biological Activities ◽  
Biological Effects ◽  
Experimental Studies ◽  
Estrogen Receptor Beta ◽  
Point Of View ◽  
Tamoxifen Treatment ◽  
Cellular Targets

Recent experimental studies revealing new biological effects of tamoxifen on tumor cells both expressing and not expressing different types of estrogen receptors (ERα and ERβ) show new aspects of a seemingly well known agent. This review describes tamoxifen targets, the blocking of which leads to inhibition of tumor cell growth and angiogenesis, stimulation of programmed cell death (apoptosis, autophagia and necrosis), inhibition of multidrug resistance, invasion and metastasis. Since outcomes of tamoxifen action on cells are prognostically good from the point of view of both tumor growth/metastasis inhibition and tumor response to drug therapy, the authors believe this is an extremely important addition to tamoxifen antiestrogenic effect. Arguments are provided to consider the strategy of long-term tamoxifen treatment proposed by Professor Craig V. Jordan in the 1970s that is also applicable to the treatment of other tumors. This is, first of all, the fact that expression of estrogen receptor-beta that can also be targeted by tamoxifen therapy in solid tumors of practically all known sites and histologies. The authors believe that molecular biological screening of patients with respect to expression of tamoxifen cellular targets other than ERα and ERβ is needed to use to the full all tamoxifen biological activities other than modulation of estrogen receptors during long-term adjuvant therapy for cancers of various sites.

Masonry: the brittle or plastic material?

2019 ◽  
pp. 22-28
Keyword(s):  
Plastic Material ◽  
Experimental Studies ◽  
Point Of View ◽  
Plastic Properties ◽  
Plastic Deformations ◽  
Base Materials ◽  
Stress States ◽  
Creep Deformations ◽  
Structural Point

The results of experimental studies of masonry on the action of dynamic and static (short-term and long-term) loads are presented. The possibility of plastic deformations in the masonry is analyzed for different types of force effects. The falsity of the proposed approach to the estimation of the coefficient of plasticity of masonry, taking into account the ratio of elastic and total deformations of the masonry is noted. The study of the works of Soviet scientists revealed that the masonry under the action of seismic loads refers to brittle materials in the complete absence of plastic properties in it in the process of instantaneous application of forces. For the cases of uniaxial and plane stress states of the masonry, data on the coefficient of plasticity obtained from the experiment are presented. On the basis of experimental studies the influence of the strength of the so-called base materials (brick, mortar) on the bearing capacity of the masonry, regardless of the nature of the application of forces and the type of its stress state, is noted. The analysis of works of prof. S. V. Polyakov makes it possible to draw a conclusion that at the long application of the load, characteristic for the masonry are not plastic deformations, but creep deformations. It is shown that the proposals of some authors on the need to reduce the level of adhesion of the mortar to the brick for the masonry erected in earthquake-prone regions in order to improve its plastic properties are erroneous both from the structural point of view and from the point of view of ensuring the seismic resistance of structures. It is noted that the proposal to assess the plasticity of the masonry of ceramic brick walls and large-format ceramic stone with a voidness of more than 20% is incorrect, and does not meet the work of the masonry of hollow material. On the basis of the analysis of a large number of research works it is concluded about the fragile work of masonry.

Nω-Hydroxy-L-arginine and Its Homologues. Chemical and Biological Properties. A Review

2004 ◽  
Vol 69 (3) ◽  
pp. 499-510 ◽  
Author(s):  
Petra Beranová ◽  
Karel Chalupský ◽  
Gustav Entlicher
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
Biological Effects ◽  
Biological Properties ◽  
No Synthase ◽  
Point Of View ◽  
No Donor ◽  
Good Substrate ◽  
No Formation ◽  
Vasorelaxant Activity

Nω-Hydroxy-L-arginine (NOHA) is a stable intermediate in NO formation from L-arginine catalyzed by NO synthase (NOS). Apparently, NOHA can be released and serve as a stable reserve NO donor (as a substrate of NOS) or transported and exert its own biological effects. It shows endothelium-dependent as well as endothelium-independent vasorelaxant activity. The latter case indicates that NOHA can be metabolized by pathways independent of NOS. These possibilities are discussed in detail. Of the available NOHA homologues homo-NOHA is a good substrate of NOS while nor-NOHA seems to be a very poor substrate of this enzyme. On the contrary, nor-NOHA exerts arginase inhibitory activity 20 times higher than NOHA whereas homo-NOHA is inactive. Detailed investigation of biological activities of NOHA and its homologues seems to be promising from the pharmacological point of view. A review with 43 references.

Abstract P130: Estrogen Receptor β Mediates the Rescue of Cardiac Function in Advanced Heart Failure by Promoting Neoangiogenesis and Reducing Fibrosis

2011 ◽  
Vol 109 (suppl_1) ◽  
Author(s):  
Andrea Iorga ◽  
Rod Partow-Navid ◽  
Humann Matori ◽  
Jingyuan Li ◽  
Soban Umar ◽  
...  
Keyword(s):  
Heart Failure ◽  
Estrogen Receptor ◽  
Estrogen Receptor Alpha ◽  
Cardiac Fibrosis ◽  
Biological Effects ◽  
Estrogen Receptor Beta ◽  
Pressure Overload ◽  
Decompensated Heart Failure ◽  
Beta Agonist ◽  
Receptor Beta

Estrogen can act via the estrogen receptor alpha (ERa) or estrogen receptor beta (ERb) to exert its biological effects, and both of these receptors are present in the heart. We have previously shown that short-term estrogen (E2) treatment can rescue pressure overload-induced decompensated heart failure (HF) in mice, and that this rescue is achieved mainly through the ERb. Furthermore, E2 has been shown to regulate angiogenesis in different tissues. Because HF has been associated with decreased angiogenesis and increased fibrosis, here we investigated whether the E2-induced rescue of HF by the selective ERb agonist DPN can regulate cardiac fibrosis and neoangiogenesis. We used transaortic constriction to induce HF, and once the ejection fraction (EF) reached ∼30%, one group of animals was sacrificed (HF group), and the other three groups received either 17b-estradiol via a subcutaneous pellet implant (0.012mg/pellet, n=16), selective ERa agonist (PPT, 0.625mg/kg/day), or selective ERb agonist (DPN, 0.625mg/kg/day) for 10 days. Serial echocardiography was performed to monitor cardiac structure and function. As expected, E2 rescued HF by restoring EF from 33.17±1.12% to 53.05±1.29%. Mice treated with DPN had a significant EF improvement from 33.17±1.12% to 45.25±2.1% (n=7), while the EF of PPT-treated mice did not improve (31.09±2.3%, n=6). Similarly, only the fractional shortening of DPN-treated mice improved from 15.7±0.58% in HF to 21.95±1.65% with DPN treatment vs. 14.72±1.24% with PPT. Next, we examined whether promotion of cardiac neoangiogenesis and suppression of fibrosis by the selective ERb agonist are possible mechanisms in the rescue action of HF by DPN. DPN treatment was able to reverse the interstitial and perivascular fibrosis observed in HF, while PPT had no effect. The selective ERb agonist also stimulated neoangiogenesis, as the capillary density was increased from 0.46±0.04 microvessels/cardiomyocyte in HF to 0.67±0.07 with DPN treatment, whereas PPT treatment had no effect (0.43±0.03). Our data strongly suggests that upregulation of cardiac neoangiogenesis and reversal of fibrosis are pivotal mechanisms in rescuing advanced HF by the estrogen receptor beta agonist DPN.

scholarly journals Effects of long-term dietary administration of estrogen receptor-beta agonist diarylpropionitrile on ovariectomized female ICR (CD-1) mice

GeroScience ◽  
2018 ◽  
Vol 40 (4) ◽  
pp. 393-403 ◽  
Author(s):  
Sherry A. Said ◽  
Rachel Isedowo ◽  
Christilynn Guerin ◽  
Navreek N. Nar ◽  
Leesa Lillie ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Beta ◽  
Beta Agonist ◽  
Receptor Beta

Estrogen Receptor Distribution in the Hippocampus and Prefrontal Cortex

2020 ◽  
pp. 11-23
Author(s):  
Annelyn Torres-Reveron ◽  
Wayne G. Brake ◽  
Teresa A. Milner
Keyword(s):  
Estrogen Receptor ◽  
Prefrontal Cortex ◽  
Estrogen Receptors ◽  
Estrogen Receptor Alpha ◽  
Estrogen Receptor Beta ◽  
Cognitive Behaviors ◽  
G Protein Coupled ◽  
The Brain ◽  
Anatomical Evidence ◽  
Estrogen Receptor 1

This chapter presents anatomical evidence for the distribution of estrogen receptors in the brain. First, the chapter presents a brief discussion of the historical findings that led to the discovery of nuclear and extranuclear estrogen receptors in the brain. A distribution pattern for each one of the receptors, estrogen receptor alpha (ERα‎), estrogen receptor beta (ERβ‎), and G-protein coupled estrogen receptor 1 (GPER1), is presented in sequential subsections. The discussion focuses on the hippocampus and prefrontal cortex areas, as these are largely involved in memory and cognitive behaviors, further discussed in other chapters in this book. In addition, co-localization studies with other neurotransmitter systems and molecules important for the functional activity of estrogen receptors is reviewed.

scholarly journals Anti-Apoptotic and Antioxidant Activities of the Mitochondrial Estrogen Receptor Beta in N2A Neuroblastoma Cells

2021 ◽  
Vol 22 (14) ◽  
pp. 7620
Author(s):  
Ioannis Tsialtas ◽  
Achilleas Georgantopoulos ◽  
Maria E. Karipidou ◽  
Foteini D. Kalousi ◽  
Aikaterini G. Karra ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Antioxidant Activities ◽  
Estrogen Receptor Beta ◽  
Direct Involvement ◽  
Neuronal Viability ◽  
Atp Production ◽  
N2a Cells ◽  
Mitochondrial Functions ◽  
Receptor Beta

Estrogens are steroid hormones that play a crucial role in the regulation of the reproductive and non-reproductive system physiology. Among non-reproductive systems, the nervous system is mainly affected by estrogens due to their antioxidant, anti-apoptotic, and anti-inflammatory activities, which are mediated by membranous and nuclear estrogen receptors, and also by non-estrogen receptor-associated estrogen actions. Neuronal viability and functionality are also associated with the maintenance of mitochondrial functions. Recently, the localization of estrogen receptors, especially estrogen receptor beta, in the mitochondria of many types of neuronal cells is documented, indicating the direct involvement of the mitochondrial estrogen receptor beta (mtERβ) in the maintenance of neuronal physiology. In this study, cell lines of N2A cells stably overexpressing a mitochondrial-targeted estrogen receptor beta were generated and further analyzed to study the direct involvement of mtERβ in estrogen neuroprotective antioxidant and anti-apoptotic actions. Results from this study revealed that the presence of estrogen receptor beta in mitochondria render N2A cells more resistant to staurosporine- and H2O2-induced apoptotic stimuli, as indicated by the reduced activation of caspase-9 and -3, the increased cell viability, the increased ATP production, and the increased resistance to mitochondrial impairment in the presence or absence of 17-β estradiol (E2). Thus, the direct involvement of mtERβ in antioxidant and anti-apoptotic activities is documented, rendering mtERβ a promising therapeutic target for mitochondrial dysfunction-associated degenerative diseases.

scholarly journals Biological effects of fulvestrant on estrogen receptor positive human breast cancer: short, medium and long‐term effects based on sequential biopsies

2015 ◽  
Vol 138 (1) ◽  
pp. 146-159 ◽  
Author(s):  
Amit Agrawal ◽  
John F.R. Robertson ◽  
Kwok L. Cheung ◽  
Eleanor Gutteridge ◽  
Ian O. Ellis ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Human Breast Cancer ◽  
Biological Effects ◽  
Human Breast ◽  
Long Term Effects ◽  
Estrogen Receptor Positive
Sign in / Sign up

Export Citation Format

Share Document