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RKI-1447 australia ELUXA HM EMSI is an ongoing
2019-12-10
ELUXA 1 (HM-EMSI-202) is an ongoing pivotal Phase II global clinical trial, designed to further investigate the efficacy and safety of Olmutinib in patients T790M-positive NSCLC with acquired resistance after first-line EGFR TKIs. Primary endpoint is ORR according to RECIST 1.1, while secondary endp
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Although the amino acid sequences
2019-12-10
Although the amino SR3335 sequences of CUL4A and CUL4B share 82% identity, the existing studies have shown that these two proteins do not have significant functional redundancy. Elevated expression of CUL4A has been observed in a variety of cancer cells, such as breast cancer, ovarian cancer, liver
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The potential off target activity
2019-12-10
The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these dat
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Epinephrine HCl receptor In frame exon skipping of COL
2019-12-09
In frame exon 41 skipping of COL6A3 has been suspected to be responsible for isolated dystonia in several human kindreds without muscular defects [94]. In order to validate their hypothesis, the authors used zebrafish to selectively knock down several exons in col6a3 and found a negative impact on m
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The Ewing sarcoma breakpoint region
2019-12-09
The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n
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ERR is present early in the developing placenta in a
2019-12-09
ERRβ is present early in the developing placenta in a subset of blasticidin in extra-embryonic ectoderm destined to make up the chorion.19, 20 ERRβ is likely essential for reproduction. ERRβ expression is essential for the maintenance of pluripotency and self-renewal potential in mouse embryonic st
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In sum although it is
2019-12-09
In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different or
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br Substrate Specificity Discrimination and Binding Energy I
2019-12-09
Substrate Specificity, Discrimination, and Binding Energy In a83 01 synthesis to catalytic efficiency, which can be gauged in reference to an absolute scale of ‘catalytic perfection’ 10, 11, specificity is a relative concept because it requires comparison between given alternative substrates. In
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In general we observed that the enolase gene with
2019-12-09
In general, we observed that the enolase gene with highest mRNA levels was TVAG_043500, under all three iron concentration conditions. mRNA levels for this gene are very similar in normal and iron rich cultures (73.9 and 78.1 fold change, respectively), and higher in iron depleted cultures (118.3 fo
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Mulan is one of three E ubiquitin ligases that are
2019-12-09
Mulan is one of three E3 ubiquitin ligases that are present in the mitochondria along with MARCH5/MITOL (membrane associated RING-CH5) and RNF185 [14], [15], [16], [17]. Mulan is a 352-residue polypeptide that crosses the mitochondrial outer membrane (OMM) twice, its amino-terminus, which includes t
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Our study showed that parental morphine
2019-12-09
Our study showed that parental morphine exposure in the adulthood is associated with an increased tendency toward morphine consumption in F1 but not F2 male offspring. Thus, it seems that trans-generational effects of parental morphine consumption disappear in the second generation. In support of ou
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Not all of the biological activities exhibited by progestoge
2019-12-06
Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the gdc-0980 is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell to respond to
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Quantum dots QDs which exhibit excellent fluorescence quantu
2019-12-06
Quantum dots (QDs), which exhibit excellent fluorescence quantum yields (QYs), high extinction coefficients and size-tunable narrow emission have highly attracted great interest in various applications such as in solar cells, sensors, and bioimaging [16], [17], [18], [19], [20]. However, QDs suffere
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br Acknowledgements This research was supported
2019-12-06
Acknowledgements This research was supported by Slovenian Research Agency (ARRS). We thank prof. R. Marinšek Logar for helpful advice, Dr. T. Kranjc for help with data management, N. Vrhovnik and G. Lavrič for technical help with preliminary growth experiments and dr. J. Burkeljca for help with g
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The attachment of ubiquitin to RTKs such as
2019-12-06
The attachment of ubiquitin to RTKs, such as EGFR, mediates efficient delivery through the endosome-lysosome system for proteolysis. In this way, RTK degradation enables cessation of signal transduction. A recent siRNA screen identified a number of USPs that can significantly modulate EGFR levels an
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