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In light of the overall loss of activity and selectivity
2021-06-03
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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br Introduction DNA dependent protein kinase
2021-06-03
Introduction DNA-dependent protein kinase (DNA-PK) is a multicomponent serine/threonine protein kinase and considered a member of the phosphatidylinositol (PI) 3-kinase related kinase (PIKK family). This enzyme plays a critical role in the repair of mammalian DNA double strand breaks (DSBs) throu
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XL-888 Then we explored the MCLEIA methodology parameters in
2021-06-03
Then, we explored the MCLEIA methodology parameters including precision, accuracy and specificity. In the 0.5–128 ng/mL, the standard curve equation was = 0.5014 + 1.769 ( was log, was RLU/RLU with a correlation coefficient of 0.9907) (). On the one hand, same sample (0.5, 4.0, 32.0 ng/mL) detected
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In this study using REMD with the crystal
2021-06-02
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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Since these first results KSTD activity has been
2021-06-02
— Since these first results, Δ1-KSTD activity has been identified in many other microorganisms, albeit sometimes with different substrate preferences. For instance, Comamonas testosteroni ATCC 11996 (formerly Pseudomonas testosteroni) is active on several steroid substrates, but it cannot use 11β-h
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Here we were able to show for the first
2021-06-02
Here, we were able to show for the first time that stimulation of VSMCs with two different growth factors resulted in a dramatic decrease in gp130mRNA expression occurring four to six hours after stimulation with Ang II and PDGF-BB. The mRNA level remained extremely low within 12 hours after stimula
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br Funding This work was supported
2021-06-02
Funding This work was supported by a research grant of the Deutsche Forschungsgemeinschaft (SCHN477-9-2 to R.S.S), the Manfred-Stolte-Stiftung (to R.S.S.) and by a research grant from the German Cancer Aid (Deutsche Krebshilfe, No. 106696/TP 5 to T.F.). Introduction Death-associated protein k
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In the context of food
2021-06-02
In the context of food allergy it is hypothesized that intestinal barrier dysfunction might contribute to both antigen sensitization and the IgE/mast cell mediated effector phase of allergic disease, however no concluding data has been published to date [5]. An understanding of the mechanism of prim
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br Chagas disease and HAT drug R D Drug
2021-06-02
Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among
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In the pleural exudates which
2021-06-02
In the pleural exudates, which reflect the in vivo conditions, the concentrations of CysLTs and PGE2 were quite similar. However, when cancer Fluconazole were cultured for 24 h, both analyses of cell culture medium and cell incubations with Ca2+ ionophore showed low levels of CysLTs. In contrast, t
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The enzyme cyclooxygenase COX or prostaglandin
2021-06-02
The enzyme cyclooxygenase (COX) or prostaglandin endoperoxide H synthase (PGHS) is the key enzyme in the conversion of arachidonic adipor1 (AA) into prostaglandins (PGs) [1]. In 1991, researchers found that there were two isoforms of this enzyme called COX-1 and COX-2 with independent genes and dif
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br Outcome of COX overexpression Although a causal role for
2021-06-02
Outcome of COX-2 overexpression Although a causal role for COX-2 has been proposed, mechanisms by which COX-2 function contributes to the pathogenesis of hyperplastic disease are not well defined. To examine if there is any correlation between COX-2 and p53 protein levels, Kumagai et al. [15] rec
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The majority of pro inflammatory cytokines are regulated by
2021-06-02
The majority of pro-inflammatory cytokines are regulated by NFκB, and recently, it has been found that p38 MAPK partly regulates NFκB-driven gene Pleuromutilin by increasing the association of the basal transcriptional factor, TATA-binding protein, with the C terminus of p65 subunit of NFκB and inc
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The immune control of CMV replication in vivo is primarily
2021-06-02
The immune control of CMV replication in vivo is primarily driven by the T-cell-mediated response, a characteristic that has been proposed as a tool to individualize and therefore to optimize antiviral treatment [6], [7], and it has been associated with spontaneous clearance of CMV viraemia in patie
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This study focused on NPC L because it is
2021-06-02
This study focused on NPC1L1 because it is critical for intestinal NAD/NADH Quantitation Colorimetric Kit of both dietary and biliary cholesterol.1, 7, 8 Overall, regulation in the intestine of cholesterol, BAs, and lipids by FGF19 and SHP may involve the combined actions of regulation of other gene
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