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Our data indicate that the ability of these promiscuous
2020-06-04
Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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br The role of chemokine and AD
2020-06-04
The role of chemokine and AD Chemokines are small cytokine proteins that are involved in various immunological and physiological functions. These proteins can be involved in cell migration and localization during homeostasis and inflammation, and as such, they were named chemokines [80]. Chemokin
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Nevertheless of the different types of scoring systems so
2020-06-04
Nevertheless, of the different types of scoring systems so far proposed, each of these [14], [29], [30] considered some aspects that could describe the fibrotic evolution, though none provided a quantitative assessment. Calvaruso et al. [8] showed that CPA had a better histological correlation with
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The desire for COTS products and some potential problems
2020-06-04
The desire for COTS products––and some potential problems There are also technological reasons in support of the use of OTS products. For example, Dawkins and Riddle (2000) point out that the relatively small safety-related systems market cannot sustain the rate of technological advancement stimula
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br Results and Discussion br Materials and Methods br Acknow
2020-06-03
Results and Discussion Materials and Methods Acknowledgements Introduction Inorganic pyrophosphate is generated as a by-product in several enzymatic reactions in cells. These reactions include DNA and RNA synthesis, activation of fatty acids and amino acids, as well as synthesis of the c
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P has three subfamilies CYP
2020-06-03
P450 has three subfamilies (CYP1, CYP2, and CYP3), which contribute largely to the oxidative biotransformation of xenobiotics that include most drugs, dietary chemicals, and environmental pollutants. The CYP1 enzymes have great importance in the bioactivation of mutagens and its isoforms are capable
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In our preliminary evaluation of this series we
2020-06-03
In our preliminary evaluation of this series, we were surprised to discover that arginase inhibitor was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is compa
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The mammalian two hybrid results
2020-06-03
The mammalian two-hybrid results described above were all obtained in 293T cells, and thus the higher RLU observed specific to the hCrm1 fusion could be consistent with human AS 101 having an unknown activator that interacts with hCrm1 HEAT repeat 9A and somehow facilitates Crm1-Rev/RRE function. Al
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br Introduction Breast cancer is the most common cancer in
2020-06-03
Introduction Breast cancer is the most common cancer in women and one of the leading causes of death worldwide. Estrogen receptor alpha (ERα, “wild-type” estrogen receptor), encoded by the estrogen receptor1 (ESR1) gene, is expressed in approximately 70% of all breast cancers. Hormonal therapy ha
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br Materials and methods br Results and discussion br
2020-06-03
Materials and methods Results and discussion Conclusions The fabrication and characterization of AMCs reinforced with SiC and RHA was done in this study. Following conclusions are drawn from the above study: Conflict of interest Authors\' contributions Introduction Industrialisati
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Similarly in the EAE model Chalmin et al previously demonstr
2020-06-03
Similarly in the EAE model, Chalmin et al. previously demonstrated that EBI2 and CH25H might be responsible for the efficient egress of differentiated Th17 cells from the draining lymph nodes [31]. As discussed above, in active EAE we did not find differences in EAE development and only the transfer
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GLP also showed cardioprotective effects i
2020-06-03
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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For example nM MTX markedly stimulates the differentiation o
2020-06-03
For example, 200nM MTX markedly stimulates the differentiation of the monocytic U937 Riociguat [39], but only 10nM MTX is sufficient for the inhibition of clonogenicity in the ALL and APL cell lines [22]. Furthermore, an even lower concentration of MTX (2nM) selectively induces the expression of p2
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DDR is one of two non integrin tyrosine
2020-06-02
DDR1 is one of two, non-integrin tyrosine kinase receptors activated by collagen. Although DDR1 has five isoforms (1a, 1b, 1c, 1d, 1e) generated by alternative splicing, only DDR1a and 1b have active kinase domains, whereas DDR2, encoded by a distinct gene, has one isoform (Vogel et al., 2006). Coll
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Of the acidic hydroxyazoles involved hydroxypyrazole had
2020-06-02
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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