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Nevertheless because of the preclinical work
2019-11-19
Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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As for the molecular mechanism Ferguson BD suggested that Ep
2019-11-19
As for the molecular mechanism, Ferguson BD suggested that EphB4/EphrinB2 stimulation induced topoisomerase I activity in small cell lung cancer cell lines. Treatment of BMI-1 inhibitor with EphrinB2/Fc induced topoisomerase activity as assessed by DNA relaxation in cells with high EphB4 expression
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br Disclosures br Acknowledgements This work was supported i
2019-11-19
Disclosures Acknowledgements This work was supported in part by grants from the Ministerio de Ciencia e Innovación, Spain (SAF2010-22051) and Xunta de Galicia, Spain (INCITE08PXIB203092PR). Introduction Ca is a key element in cardiac excitation–contraction (EC) coupling. In each heartbeat,
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The synthetic route chosen for the preparation
2019-11-19
The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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Another interesting finding regarding substrate selectivity
2019-11-19
Another interesting finding regarding substrate selectivity of iPLA2-VIA in whole cellular systems stems from the observation that some of the major species hydrolyzed by the enzyme contain a 16:1 fatty inositol phosphatase at the sn-2 position [57,119], raising the possibility that iPLA2-VIA may c
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E ligases provide substrate recognition specificity Ubiquiti
2019-11-19
E3 ligases provide substrate recognition specificity Ubiquitination ppy and substrate specificity in mammals is achieved by the existence of over six-hundred E3-ubiquitin ligases that catalyze the final step of ubiquitination, compared with only one E1 and very few E2 enzymes known till date [23].
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br RING type E s and their substrates There
2019-11-19
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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Dysfunction of the ubiquitin proteasome system causes abnorm
2019-11-19
Dysfunction of the ubiquitin-proteasome system causes abnormal organelle morphology and impairs sperm formation and maturation steps resulting in male infertility [[7], [8], [9]]; this indicates that ubiquitination is essential for spermatogenesis and sperm function during fertilization. β-catenin i
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br Patients and Methods Patients who had been
2019-11-19
Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl)
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The number of DBH alleles affects dopamine
2019-11-19
The number of DBH MYK-461 affects dopamine and norepinephrine levels in the prefrontal cortex of mice when they are treated with disulfiram (33). Disulfiram increased dopamine and decreased norepinephrine levels in their prefrontal cortex of mice with two normal alleles, whereas disulfiram showed re
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The second part of this study evaluated the role of
2019-11-18
The second part of this study evaluated the role of CK1 in the eFABP4 cellular uptake in endothelial cells. By blocking CK1 expression using a specific siRNA, we corroborated that the presence of CK1 was fundamental for FABP4 cellular uptake and internalization in endothelial cells, thus decreased m
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As before all calculations are based on thermodynamically
2019-11-18
As before [3], [4], all calculations are based on thermodynamically first- and second-order hydropathic (amino acid) scales [6], [7], linearly scaled to a common center and a common range for each of the 20 amino acids. These are then converted to a triangular matrix , where is the length of a sli
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4μ8C mg To investigate the role of DPP inhibition in inflamm
2019-11-18
To investigate the role of DPP-4 inhibition in inflammation-induced bone resorption, we evaluated the effect of a DPP-4 inhibitor on LPS-induced osteoclast formation and bone-resorption in vivo. Our results showed that the DPP-4 inhibitor inhibited LPS-induced osteoclast formation and bone resorptio
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Autophagy alterations are frequently reported as one of the
2019-11-18
Autophagy alterations are frequently reported as one of the pathological mechanisms contributing to neurodegenerative diseases, due to incomplete removal of protein R547 in the brain [30,41]. It was over a decade ago when mutations in PARK8 encoding for the LRRK2 protein were described as a main ge
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Altogether the results of this study demonstrate that periph
2019-11-18
Altogether, the results of this study demonstrate that peripheral blockade of both ETA and ETB receptors reduces tumor-induced facial heat hyperalgesia and increased spontaneous grooming, without modifying ongoing nociception. It is possible to suggest that bosentan is acting upon both receptors pre
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