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We hypothesized that the atopic phenotype
2020-02-11

We hypothesized that the atopic phenotype may be partially influenced by an altered binding and/or signalling due to the amino-acid substitution in the receptor protein. The principal aim of this study was to investigate the signalling mechanisms of the variants CysLT1-G300S and CysLT1-I206S induced
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Although it is believed that CYP induction
2020-02-11

Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)
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As the principal receptors for regulating the inflammatory
2020-02-11

As the principal receptors for regulating the inflammatory process in mammals, CXCR1 and CXCR2 have an important role in regulating the trafficking of phagocytes such as neutrophils, monocytes and macrophages (Viola and Luster, 2008). The evidence gathered to date from fish studies are in agreement
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An ideal CHK inhibitor would be
2020-02-11

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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Building s constructional elements should be able to protect
2020-02-11

Building\'s constructional elements should be able to protect residents from the negative effect of noise caused by surroundings [19]. The World Health Organization estimates that each year more than one million Healthy Life Years are lost in the European Union member states and other Western Europe
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Although DGK is a lipid modulating enzyme the role
2020-02-10

Although DGKγ is a lipid-modulating enzyme, the role of DGKγ in integral cell metabolism has not been reported. We found that DGKγ made a difference on cell metabolism profile in HCC cells, which may be caused partially by the downregulation of GLUT1. Glucose is a major source of energy, and decreas
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In conclusion DDR ECD was shown to
2020-02-10

In conclusion, DDR1 ECD was shown to be sufficient for collagen mediated DDR1 oligomerization, and the oligomerized form binds to collagen with increased affinity. In full length receptors expressed on live cells, DDR1 oligomerization occurred on the cell surface in agreement with the role of DDR1 E
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The CRTH inhibitory activities of the synthesized compounds
2020-02-10

The CRTH2 inhibitory activities of the synthesized compounds are listed in , . At first we introduced halogen or other substituents at the 4,4′-position of phenyl rings in the benzhydryl moiety in order to obtain SAR and to improve the metabolic stability at this moiety (–). It is well-known that in
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Interestingly ASV infusion in the dRN
2020-02-10

Interestingly, ASV-30 infusion in the dRN of saline pre-treated rats had no effect on anxiety-like behaviors. This result may be due to the saline pre-treated group exhibiting relatively low levels of anxiety-like behaviors (when compared to saline pre-treated rat of the first experiment that were n
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Emi protein consists of an N terminal
2020-02-10

Emi2 protein consists of an N-terminal regulatory region and a C-terminal functional region. The C-terminal region contains a destruction box (D-box), which likely competes with APC/C substrates (including cyclin B) for APC/C binding, and a zinc-binding region (ZBR), which somehow inhibits APC/C ubi
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br Benefits and risks of traditional combined oestrogen prog
2020-02-10

Benefits and risks of traditional combined oestrogen–progestogen HRT regimens Combined oestrogen–progestogen regimens were developed to reproduce the short- and long-term benefits of oestrogen replacement therapy (ERT) and to simultaneously provide appropriate protection against oestrogen-related
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Among RAS mutant tumors analyzed we found that
2020-02-10

Among RAS mutant tumors analyzed, we found that the efficacy of either the SHP2 inhibitor SHP099, or combined MEK and SHP2 inhibition was best in those expressing RAS mutations at G12 (Figure 7B). Recent studies revealed that cellular RAS(G12C) activity depends on RTK-mediated nucleotide exchange, a
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Because EBI is expressed on the major subsets of
2020-02-10

Because EBI2 is expressed on the major subsets of immune cells, and small molecule antagonists for EBI2 were recently described (Benned-Jensen et al., 2013, Gessier et al., 2014), EBI2 constitutes a tempting drug target reminiscent of the sphingosine-1-phosphate receptor superagonist fingolimod/Gile
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Here we discuss implications of several major
2020-02-10

Here, we discuss implications of several major families of RING-type E3 ubiquitin ligases (MDM, Cullin, GRAIL, TRAF, TRIM) as targets in inflammation and immunity, and provide insights into potential small molecule interventions to mediate the cellular responses (summarized in Table 1). We briefly c
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Several eukaryotic E enzymes including
2020-02-10

Several eukaryotic E3 enzymes, including BRE1 [49], RNF8 [50], and RAD18 [24], [51], have been reported to partner with UBE2B in the ubiquitination of various targets. We examined the expression levels of these E3 enzymes in HONE1 and TW01 cells; RAD18 was highly expressed in these DL-Dithiothreito
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