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BLZ945 TKI discontinuation studies demonstrate that
2020-12-09
TKI discontinuation studies demonstrate that a portion of TKI-treated CML patients remain in remission for up to 3 years, although long-term risk assessment is still necessary (Bansal and Radich, 2016). The majority of CML patients depend on lifetime TKI treatment, and substantial efforts have been
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In order to evaluate the in
2020-12-09
In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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There has recently been some interest in Uba which
2020-12-09
There has recently been some interest in Uba6, which is most similar to slime mold, with BLAST identities of 59% and positives 73% in the 400–600 ADD range. The 400–600 ADD correlation of the two profiles is a striking 87%, so functional differences probably arise outside the ADD binding domain. Hu
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Regarding eicosanoid production iPLA VIA appears in general
2020-12-09
Regarding eicosanoid production, iPLA2-VIA appears, in general terms, not to play a major role in mediating this response in innate immunity and inflammation, as evidenced by the large number of studies highlighting the lack of effect of selective inhibition of the enzyme in stimulus-induced AA rele
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The role of ETB clearing receptors has been studied in
2020-12-09
The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous ll-37 mg of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all other c
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The discovery of proteases that are active in
2020-12-09
The discovery of proteases that are active in organic solvent media has greatly extended their ability in the synthesis of useful products. Microbial proteases which are able be catalyse in non-aqueous solvents present new expectation in enzyme applications. This kind of enzymes gives a major contri
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br Perspective and conclusion Collagen Toolkits II and
2020-12-09
Perspective and conclusion Collagen Toolkits II and III have been used to determine the Repaglinide for DDR1 and DDR2, and the main binding site is the GVM-GFO motif [103,108]. The co-crystal structure of the DS domain of human DDR2 bound to a synthetic collagen-like peptide containing the GVM-G
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CYP A and CYP D are
2020-12-09
CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i
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br Materials and methods br Results br
2020-12-09
Materials and methods Results Discussion In addition, the responses of CYP450s induced by metalaxyl are species-specific in the four cells. For example, metalaxyl lead to induction of CYP1A1, CYP1A2, and CYP2B1 in HepG2 cells, CYP1A2 and CYP2B1 in H4IIE cells, CYP1A1 and CYP2B1 in LMH cells
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A study profiling chemokine expression
2020-12-09
A study profiling chemokine expression in LCLs revealed high expression levels of CCR6, CCR7, and CCR10 and low expression of CXCR4 and CXCR5 in EBV immortalized cells. Accordingly, LCLs showed a markedly increase in migration in response to the ligands of CCR6 (CCL20), CC7 (CCL21), and CCR10 (CCL28
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The important role of miRNAs in cellular differentiation
2020-12-08
The important role of miRNAs in cellular differentiation has been proposed recently. Previous studies had suggested roles for different miRNAs during osteogenesis [20]. Certain miRNAs could promote osteoblast differentiation, such as miR-194 [20], whereas others could inhibit the cell differentiatio
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indacaterol australia We also observed reduced insulinotropi
2020-12-08
We also observed reduced insulinotropic effects after intravenous administration of both GLP-1 and GIP with atropine, whereas no inhibition was observed by atropine of the direct effects of GLP-1 and GIP action on beta-cells in the islet experiments. This suggests that the reduction in circulating i
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verubecestat Another mechanism underlying on the toxicity of
2020-12-08
Another mechanism underlying on the toxicity of dopaminergic neurons might be related to dopamine-dependent initial oxidative stress [60]. Dopamine verubecestat mediated by monoamine oxidase (MAO) can produce hydrogen peroxide as a by-product, and excess dopamine can undergo auto-oxidation to quino
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In this study using REMD
2020-12-08
In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).
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The body wall intestine seminal receptacle and
2020-12-08
The body wall, intestine, seminal receptacle and seminal vesicle in the adult worms were also isolated and homogenized to make microsomal fractions to investigate the relative expression of CYP1A2, CYP2E1 and CYP3A4 in these different organs. In order to get sufficient mass, about 20 individual adul
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