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br Materials and methods br Results br Discussion
2019-09-19

Materials and methods Results Discussion TP has aroused extensive explorations because of its potent anti-inflammatory, immune-suppressive and antitumor activities. Notwithstanding these, TP has yet to enter Phase II clinical trials owing to its severe toxicity (Zhou et al., 2012). TP could
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In a previous study we reported that
2019-09-19

In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in MLCK inhibitor peptide 18 kinase reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present exp
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br Acknowledgments br Multicellular organisms respond rapidl
2019-09-18

Acknowledgments Multicellular organisms respond rapidly, and adapt to cellular stress to maximize cell survival. The cellular stress response, also called (ISR), is universally conserved and independent of the stressor. ISR induces rapid, transient reprogramming of cellular protein translation
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Colony stimulating factor receptor CSF R or cFMS is a
2019-09-18

Colony stimulating factor-1 receptor (CSF-1R or cFMS) is a type III receptor tyrosine kinase. It is activated by binding with CSF-1 and IL-34, which stimulates differentiation, proliferation, survival and migration of monocyte-macrophage lineage cells., , , Also, macrophages produce inflammatory me
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From the general synthetic route we first synthesized
2019-09-18

From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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Given that dimethylamine substitution was tolerated
2019-09-18

Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated Mithramycin A amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The
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Febuxostat To study systemic potential of the selected compo
2019-09-18

To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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Coumarins also known as benzopyran ones are a
2019-09-17

Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. Ov
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Previously published data showed an interaction
2019-09-17

Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino pdgf receptor sequence (Suppl
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br Clinical studies br Practical implications for young
2019-09-17

Clinical studies Practical implications for young women Conclusion Research on the oncogenic mechanism of hormones has advanced dramatically in the latter years. The finding that progestogens are more powerful determinants of risk than estrogens in breast cancer has been added to advances i
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Arsenic is an endocrine disruptor with estrogenic activity
2019-09-17

Arsenic is an endocrine disruptor with estrogenic activity. Further study has shown that arsenic exposure can significantly increase the expression of estrogen receptor-related genes, steroid metabolism-related enzymes and lung cancer-related genes in the lung tissues of female mice on the occurrenc
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br Materials and methods br Results
2019-09-17

Materials and methods Results Discussion It has been demonstrated that up-regulation of EPHB4 impaired trophoblast migration and invasion during placentation, which may contribute to the pathogenesis of preeclampsia [11], [24]. However, the upstream regulating mechanism of EPHB4 expression
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The most significant finding was the
2019-09-17

The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using
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br Acknowledgments The authors acknowledge funding from the
2019-09-17

Acknowledgments The authors acknowledge funding from the National Key Research and Development Program of China (2016YFA0502900) and the National Science Foundation of China (31570188). Compartment Size Regulation Regulation of compartment size is one of the most fundamental issues in biology
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Analysis of Table shows that compound b in
2019-09-17

Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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