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Although the expression of EGFR was reported
2020-07-27
Although the expression of EGFR was reported to be upregulated by hypoxic conditions in breast, non-small-cell lung, cervical and head and neck cancers, some recent researches demonstrated that EGFR was significantly downregulated in hypoxic areas of the head and neck cancer (Mayer et al., 2016). EG
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DNA PK plays an essential role in protecting genome
2020-07-27
DNA-PK plays an essential role in protecting genome stability during the events of double-strand break (DSB), and considered crucial component in NHEJ repair pathway. Where, in such pathway, DNA-PKcs is recruited at the site of DSB by the Ku protein, which in turn recruits and phosphorylates a nucle
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The binding of collagen X to DDR differs
2020-07-27
The binding of collagen X to DDR2 differs from the binding of collagen X to α2β1 integrin in that the triple helical conformation is essential for DDR2 binding. We previously reported that heat denatured pepsinised collagen X supported cell adhesion via α2β1, indicating that the triple-helical confo
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Several putative sites in the discoidin
2020-07-27
Several putative sites in the discoidin (DS) domain, DS-like domain and the JM region of DDR1 ECD may mediate oligomerization of DDR1-Fc dimers. In a recent study, Carafoli et al. (2012) have shown that monoclonal kinesin 5 (mAbs) that bind to the DS-like domain of DDR1, inhibit collagen-induced re
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LY2409881 br Conclusions Present work comprehensively charac
2020-07-27
Conclusions Present work comprehensively characterizes the inhibitory activity of Yersinia enterocolitica against cysteine proteases. All tested strains, regardless of their bioserotype, LY2409881 and the presence of virulence markers, synthesized the high-molecular-weight inhibitors of papain an
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Culture conditions particularly temperature which affect the
2020-07-27
Culture conditions (particularly temperature), which affect the pathogenicity of Y. enterocolitica (Bottone, 1997), may also impact its inhibitory properties against cysteine proteases. However, culturing the bacterial strains at 37 instead of 28 °C did not alter remarkably the inhibitory potential
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Although it is believed that CYP induction is regulated
2020-07-27
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 Linezolid induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PC
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Six substrate recognition sites SRS SRS
2020-07-27
Six substrate recognition sites (SRS1-SRS6) have been identified at positions 102-123, 204-209, 238-244, 301-319, 374-382 and 483-492 (Table 2, underlined residues) based on Gotoh\'s proposal [30]. CYP3A163 displays the similar characteristic long sequences between helices F and G presenting two add
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The teleost CXCL CXCR system serves as
2020-07-27
The teleost CXCL12-CXCR4 system serves as an ideal model to study the subfunctionalization of duplicated genes (He and Zhang, 2005). The two zebrafish CXCL12 genes have diversified their functions in concert with the two receptors, to generate relative specificity of ligand/receptor binding (CXCL12a
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PGD binds to three different receptors the prostaglandin
2020-07-27
PGD2 binds to three different receptors: the prostaglandin D2 receptor or DP (also known as DP1) [12], the chemoattractant receptor-homologous molecule expressed on Th2 cells or CRTh2 (also known as DP2) [13] and the thromboxane-type prostanoid receptor (TP), although at higher concentrations [14],
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The pharmacokinetics properties of compound were
2020-07-27
The pharmacokinetics properties of abk were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability (38%
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br Methods br Results br Discussion The
2020-07-25
Methods Results Discussion The lowest intra-CeA dose of R278995/CRA0450 that prevented the elevations in prostanoid receptors reward thresholds associated with nicotine withdrawal was 0.05μg/side (0.1μg total bilateral dose). The total bilateral dose in the present study is 100 times lower
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As the COMT enzyme is primarily related to prefrontal
2020-07-25
As the COMT enzyme is primarily related to prefrontal dopamine degradation (e.g., Yavich et al., 2007), the present study supports the notion that prefrontal dopamine modulates retention of fear extinction rather than within-session extinction (Abraham et al., 2014). Consistent with other studies we
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The binding pattern of was analysed by flexible molecular do
2020-07-25
The binding pattern of 1 was analysed by flexible molecular docking. The Leupeptin inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with the side chains residues of Ile95, Met
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As expected the nortestosterone derived
2020-07-25
As expected, the 19-nortestosterone-derived progestins tested were moderate agonists of hAR (C), with EC50s ranging from 2 to 10nM, however all were less potent than the endogenous ligand DHT by at least a factor of 6, with relative potencies ranging from 0.0301 to 0.164. This is in agreement with p
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