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Interestingly our analyses of human
2019-07-10
Interestingly, our analyses of human PBMCs using a monoclonal antibody against EBI2 showed that the expression pattern of human EBI2 is largely overlapping with that in mice. Especially Th17 bcr-abl inhibitor showed homogeneous high expression of EBI2 compared with Th1 cells, which contained a fract
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Imatinib STI is a first line tyrosine kinase inhibitor TKI
2019-07-10
Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF
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br Results and Discussion br Conclusions Based on their comm
2019-07-10
Results and Discussion Conclusions Based on their common NTP pyrophosphatase activity, similar size of the catalytic domains, and the conservation of glutamate residues, it was assumed previously that the MazG and HisE families were related to MutT and other Nudix family hydrolases (see Zhang
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The presence of H PPases
2019-07-10
The presence of H+-PPases in parasitic protists raises the question of the physiological role of these proteins. So far, they had been extensively characterized mainly in higher plants, and some prokaryotes [1], [2], [3], [4], [5], [6], [7], [16], [20]. A common feature to all these organisms is tha
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To simulate the inhibition of the enzyme by organophosphorus
2019-07-10
To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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By using the C elegans
2019-07-10
By using the C. elegans Matrisome Annotator tool, we found substantial enrichment for matrisome Istradefylline in these data sets. Thus, re-analyzing -omic datasets with the C. elegans Matrisome Annotator tool may be useful to generate novel hypotheses about the role of the C. elegans matrisome for
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Introduction Hepatocarcinoma is a common and aggressive form
2019-07-10
Introduction Hepatocarcinoma is a common and aggressive form of cancer (Trad et al., 2017). Due to a high rate of postoperative recurrence and metastasis, the prognosis for HCC remains dismal (Wang et al., 2017a, 2017b). Subclinical metastasis is the major cause responsible for tumor recurrence and
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br Materials and methods br Results br Discussion A reporter
2019-07-10
Materials and methods Results Discussion A reporter of FGF signaling activity has long been sought to facilitate the quantitative real-time analysis of pathway activity at single-cell resolution. Here we report the generation of a Spry4 reporter allele in ESCs and mice that recapitulates kn
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Oysters belong to the second largest animal phylum Mollusca
2019-07-09
Oysters belong to the second largest animal phylum Mollusca, and they are globally distributed aquaculture animals (Wang et al., 2018). A number of studies have demonstrated that oysters have evolved an integrated and complex innate immune system to recognize and eliminate various invaders. An array
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DDR is characterized by an N terminal discoidin domain
2019-07-09
DDR2 is characterized by an N-terminal discoidin domain and a C-terminal kinase domain [7]. Characteristics of DDR1, which is a homologue of DDR2, have been extensively investigated in terms of expression level in cancer tissues and biological functions in normal and cancer cell conditions, but char
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Recently roflumilast has been approved
2019-07-09
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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Enolases are among the most abundantly expressed
2019-07-09
Enolases are among the most abundantly expressed cytosolic proteins. They are metalloenzymes that catalyze the conversion of 2-phosphoglycerate to phosphoenolpyruvate [18]. Eubacteria and archaebacteria have a single enolase gene (reviewed in [19]). Despite the lack of signal peptides or cognate pr
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br Restenosis after angioplasty remains a remarkable
2019-07-09
Restenosis after angioplasty remains a remarkable challenge, although drug-eluting stents have reduced the incidence of restenosis considerably . Vascular smooth muscle M 1145 molecular (VSMCs) play a pivotal role in the development of intimal thickening and restenosis. VSMCs proliferate and migr
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In light of the overall loss
2019-07-09
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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For the SAR optimization of the right
2019-07-09
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic BMS 193885 what moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by cond
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