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It is now well accepted that increased
2020-12-21
It is now well accepted that increased local estrogen levels are associated with both the onset and growth of breast cancer. Tissue concentrations of estradiol (E2) in breast cancer are 10 times higher than that found in plasma [12]. Breast cancer tissues also contain increased activity and expressi
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The synthesis of the required substrates is shown in
2020-12-18
The synthesis of the required substrates is shown in (see for experimental details). Treatment of heterocycle with Cabazitaxel under basic conditions afforded a mixture of the mono-substituted product (22%) and the di-substituted compound (38%) which were separated by column chromatography. C
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Ademetionine Both receptors belong to the
2020-12-18
Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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The biological actions of ET are mediated via two
2020-12-18
The biological actions of ET‐1 are mediated via two distinct receptor subtypes, the endothelin A and endothelin B receptors (ETA/ETB). While activation of ETA is assumed to mediate contraction of smooth muscle cells, the activity of ETB is related to transient vasodilation [22]. In human corpus cave
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Bay 65-1942 HCl salt GLP also showed cardioprotective effect
2020-12-18
GLP-1 also showed cardioprotective effects (i.e., infarct size reduction and ejection fraction improvement) in experimental models of myocardial ischemia-reperfusion injury by suppressing caspase-3 activation and preventing apoptosis of cardiomyocytes [[50], [51]]. Of note, such a cardioprotection w
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Although the implication of DA and glutamate signaling cross
2020-12-18
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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If the unwanted objects detected by OpenComet are manually d
2020-12-18
If the unwanted objects detected by OpenComet are manually deleted, and then the DNA (%) in tail is computed, the performance of the present method can be compared more effectively. Therefore, performance of OpenComet is analysed in two ways as Approach 1 and Approach 2. Approach 1, considers the DN
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The sixth affected individual individual is
2020-12-18
The sixth affected individual (individual 6) is a 35-year-old female who presented with a complex combination of congenital and acquired symptoms. She was born to healthy, unrelated parents with an unremarkable family history, apart from the presence of polycystic kidney disease in her father and pa
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Madecassic acid In recent years the use of liquid
2020-12-17
In recent years, the use of liquid chromatography/tandem mass spectrometry (LC–MS/MS) has become a preferred approach to measure drugs and metabolites in biological fluids due to its very high selectivity and sensitivity [17], [18], [19], [20], [21], [22], [23], [25], [30]. The great sensitivity of
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br Results br Discussion SDF performs essential roles in cel
2020-12-17
Results Discussion SDF-1 performs essential roles in cell migration and proliferation, acts as neuromodulator; and is also involved in many pathological processes including human immunodeficiency virus infection, metastatic malignancy, and chronic inflammatory disorders (Feng et al., 1996, Li
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The corticotropin releasing factor CRF also referred to as c
2020-12-17
The corticotropin-releasing factor (CRF) also referred to as corticotropin-releasing hormone, is a key mediator of mammalian endocrine, behavioral, autonomic, and immune responses to stress (Vale et al., 1981, Owens and Nemeroff, 1991, Bale and Vale, 2004). Within the hypothalamic–pituitary–adrenal
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In our ongoing investigation of the
2020-12-17
In our ongoing investigation of the structure activity relationship of benzenesulfonamide anti-inflammatory activity, we designed and synthesized a novel set of benzenesulfonamide derivatives starting from commercially available sodium saccharin. The pivotal features of our approach aimed to do some
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The substitution of serine by an alanine
2020-12-17
The substitution of serine 185 by an alanine led to an increase of EGF-R stabilization along with a better binding of PRK1, a RhoB effector described to be involved in EGF-R intracellular traffic. Overall these data indicated that the phosphate group on serine 185 impaired its binding to the effecto
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An ideal CHK inhibitor would be
2020-12-17
An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th
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Hepatocyte proliferation is accompanied by changing gene exp
2020-12-17
Hepatocyte proliferation is accompanied by changing gene expression [1,2]. as two of the three estrogen receptors are transcription factors: Estrogen Receptor alpha (ERα) and ERβ [[3], [4], [5]]. The most potent ligand estradiol, binds to ERα/ERβ and exerts changing cognate gene transcription [5]. O
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